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Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms .
M1/M4 muscarinic agonist 1 (compound 41) is a selective muscarinic M4/M1 agonist with EC50 values of 14 and 55 nM for M4 and M1, respectively. M1/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusional disorder, etc .
M1/M2/M4 muscarinic agonist 1 (Compound 42) is a muscarinic M4/M1/M2 agonist with EC50 values of 6.5, 26 and 210 nM for M4/M1/M2, respectively. M1/M2/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusion, etc .
PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively . Antidyskinetic effect.
McN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 reduces inflammation and oxidative stress in an experimental model of ulcerative colitis . McN-A-343 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo .
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .
L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
L-Hyoscyamine sulfate hydrate, a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate hydrate is a levo-isomer to Atropine (HY-B1205) .
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively .
L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
Thiochrome (Standard) is the analytical standard of Thiochrome. This product is intended for research and analytical applications. Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
Xanomeline (LY 246708) is the potent agonist of muscarinicM1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .
Anisotropine (Octatropine) bromide is an orally active anticholinergicmuscarinic antagonist. Anisotropine bromide can inhibit gastric acid secretion and is used as an adjunct to peptic ulcers .
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect .
GEA 857 is a structural analog of the Serotonin (HY-B1473A) uptake blocker Alaproclate (HY-164011). GEA 857 enhances responses induced by muscarinic receptor agonists by inhibiting certain calcium-dependent potassium channels on membranes, a blockade that can enhance or prolong the muscarinic cholinergic effects. GEA 857 can be used in research on neurodegenerative diseases .
L-Hyoscyamine (Standard) is the analytical standard of L-Hyoscyamine. This product is intended for research and analytical applications. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
Darotropium bromide (GSK233705), a long-acting muscarinic antagonist and an inhaled anticholinergic, can be used for the research of chronic obstructive pulmonary disease (COPD) .
Trihexyphenidyl is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
SCH 211803 is a selective antagonist of the M2muscarinic receptor. SCH 211803 is promising for research of cardiovascular and nervous system diseases .
Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
AZD-9164 (bromide) is a long-acting muscarinic M3 antagonist. AZD-9164 (bromide) is promising for research of airways diseases, such as chronic obstructive pulmonary disease (COPD) or asthma .
(±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits α-adrenergic receptor activity. (±)-Scopolamine has Ki values of 33 μM and 7.25 nM for α1-adrenerg receptor and muscarinic cholinergic receptor, respectively .
L-Hyoscyamine (sulfate) (Standard) is the analytical standard of L-Hyoscyamine (sulfate). This product is intended for research and analytical applications. L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases .
AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
PF-3635659 is a potent antagonist of the muscarinic M3 receptor (mAChR3). PF-3635659 can be used for chronic obstructive pulmonary disease (COPD) research .
LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC50 of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research .
Trihexyphenidyl (hydrochloride) (Standard) is the analytical standard of Trihexyphenidyl (hydrochloride). This product is intended for research and analytical applications. Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
(Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .
Sofpironium (BBI 4000) tosylate is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium tosylate reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium tosylate also has a high afnity for the M1, M2, M4 and M5 subtypes .
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes .
Tropicamide (Ro 1-7683) is a selective M4muscarinic acetylcholine receptor antagonist. When used as an eye drop, Tropicamide causes short-term mydriasis (pupil dilation) and cycloplegia. Tropicamide can be used in the research of neurological diseases, such as epilepsy .
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia .
Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride hydrate potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride hydrate can be used for the research of parkinsonian .
Metixene (Piperidine) is an anticholinergic and antiparkinsonian agent. Metixene potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene can be used for the research of parkinsonian .
Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride can be used for the research of parkinsonian .
THRX-195518 is the major metabolite of Revefenacin (HY-15851), a lung-selective and long-acting muscarinic antagonist. THRX-195518 can be utilized in research related to chronic obstructive pulmonary disease .
Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .
Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .
3-Hydroxy darifenacin is a metabolite of Darifenacin (HY-A0033). 3-Hydroxy darifenacin is an antagonist of M1-5muscarinic receptors with Kis values of 17.78, 79.43, 2.24, 36.31 and 6.17 nM, respectively in CHO cells .
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .
Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder .
BAY-2413555 is an orally active muscarinic acetylcholine receptor M2 modulator that protects the heart and improve cardiac function. BAY-2413555 is promising for research of heart failure .
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR .
Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine hydrochloride is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki= 84 nM, M1 receptor) and low (Ki= 1.65 μM, M2 receptor) affinity sites [1]. Oxomemazine hydrochloride an antihistamine and anticholinergic agent used for the study of cough treatment .
Arecoline hydrochloride, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrochloride exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrochloride also can induce oxidative stress .
Arecoline, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress .
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .
Procyclidine (hydrochloride) (Standard) is the analytical standard of Procyclidine (hydrochloride). This product is intended for research and analytical applications. Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
Metixene (hydrochloride hydrate) (Standard) is the analytical standard of Metixene (hydrochloride hydrate). This product is intended for research and analytical applications. Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent. Metixene hydrochloride hydrate potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene hydrochloride hydrate can be used for the research of parkinsonian .
Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinicmAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinicmAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
Anisodamine (6-Hydroxyhyoscyamine), a belladonna alkaloid, is a non-subtype-selective muscarinic, and also a nicotinic cholinoceptor antagonist. Anisodamine employs in traditional Chinese medicine for many ailments, mainly to improve the microcirculation in states of shock, and also in organophosphate poisoning .
β2AR agonist /M-receptor antagonist-1 is a potent dual muscarinic antagonist/beta 2 agonist (MABA). β2AR agonist /M-receptor antagonist-1 potently relaxes either Carbachol (HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol (M3; HY-B1208), or Histamine (HY-B1204)-induced contraction (β2) .
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence .
Anisodamine (hydrobromide) (Standard) is the analytical standard of Anisodamine (hydrobromide). This product is intended for research and analytical applications. Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline can cross the blood-brain barrier (BBB) .
Flavoxate (hydrochloride) (Standard) is the analytical standard of Flavoxate (hydrochloride). This product is intended for research and analytical applications. Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
Aclidinium is a long-acting muscarinic antagonist and long-acting β2-adrenoceptor (β2-AR) agonist with bronchodilator activity. Aclidinium can reduce hyperinflation of the lungs and increase lung function and exercise endurance time. Aclidinium is used in research on chronic obstructive pulmonary disease (COPD) .
Arecoline (hydrobromide) (Standard) is the analytical standard of Arecoline (hydrobromide). This product is intended for research and analytical applications. Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
M1 ligand 1 (compound 3b-b) is a muscarinic acetylcholine receptor M1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer .
TAAR1 agonist 2 (compound 30) is a full agonist of trace amine-associated receptor 1 (TAAR1) (pEC50=7.5). TAAR1 agonist 2 also exhibits agonist activity at H1 receptors and activates several members of the muscarinic acetylcholine receptor family, such as the M2 receptor (pEC50=5). TAAR1 agonist 2 can be used in the study of neuropsychiatric diseases .
Mepenzolate bromide is an orally administered muscarinic receptor antagonist with Kis of 0.68 and 2.6 nM for hM2R and hM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome .Mepenzolate bromide is a GPR109A inhibitor .
Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
Oxomemazine (Standard) is the analytical standard of Oxomemazine. This product is intended for research and analytical applications. Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
AE9C90CB, muscarinic receptor antagonist, has greater affinity for M3 muscarinic receptors with pKi of 9.90 and was 20-fold more selective for M3 than for M2 muscarinic receptors .
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
Aceclidine (Quinuclidin-3-yl acetate) hydrochloride is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC50: 40 μM). Aceclidine hydrochloride is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine hydrochloride has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
Peimisine (Ebeiensine) hydrochloride is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine hydrochloride shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research .
Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research .
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .
UH-AH 37 is a muscarinic (mAChR) antagonist. UH-AH 37 exhibits a higher potency in inhibiting muscarinic responses in intestinal tissue than cardiac tissue .
L-687306 is a high affinity muscarinic M1 receptor partial agonist with activity as a partial agonist of M1 receptors in rat ganglia and as a high affinity competitive antagonist at guinea pig cardiac M2 and ileal M3 muscarinic receptors, useful for studying the receptor reserve of muscarinic receptors.
DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
Scopolamine hydrochloride is a non-selective and high affinity (≤1 nM) muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. Scopolamine readily passes the blood brain barrier. Scopolamine also reversibly inhibits 5-HT3 receptor-responses with an IC50 of 2.09 μM . Scopolamine induces Alzheimer's disease-like pathology through alteration of cholinergic system .
Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
AQ-RA 721 is a muscarinic receptor antagonist with differential affinity for the m4 and M2 sites, which can be used to characterize muscarinic receptor subtypes. Other muscarinic receptor antagonists have differential affinity for the M1 (rat cerebral cortex), M2 (rat heart), M3 (rat submandibular gland), m4 (receptor expressed in Chinese hamster ovary cells transfected with CHO), and guinea pig uterine smooth muscle at the muscarinic binding site .
Cyclopentolate (DL-Cyclopentolate) is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate is an anti-muscarinic agent commonly used in the ophthalmologic practice .
Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice .
Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca 2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca 2+]i .
Pilocarpine (Hydrochloride) (Standard) is the analytical standard of Pilocarpine (Hydrochloride). This product is intended for research and analytical applications. Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
Peimisine (Standard) is the analytical standard of Peimisine. This product is intended for research and analytical applications. Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research .
Pilocarpine (nitrate) (Standard) is the analytical standard of Pilocarpine (nitrate). This product is intended for research and analytical applications. Pilocarpine nitrate is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
Cyclopentolate (hydrochloride) (Standard) is the analytical standard of Cyclopentolate (hydrochloride). This product is intended for research and analytical applications. Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice .
Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease .
Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011), a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
Biperiden (hydrochloride) (Standard) is the analytical standard of Biperiden (hydrochloride). This product is intended for research and analytical applications. Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance [4].
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
Acetylcholine iodide is a muscarinic receptor modulator. Acetylcholine iodide specifically binds to muscarinic receptors, inhibits sodium absorption, and induces chloride secretion. Acetylcholine iodide changes intestinal ion transport, enhances intestinal secretory function, induces or maintains mammary gland development and lactation. Acetylcholine iodide can be used for intestinal ion transport regulation and mammary gland physiological function research .
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4].
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist .
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride[1]. Tolterodine hydrochloride is a potent muscarinic receptor antagonist[2][3].
Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM) .
Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
DAU 5884 hydrochloride is a potent muscarinic M3 receptor antagonist. DAU 5884 hydrochloride inhibits methacholine-dependent effects on cell proliferation and muscle contractility .
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Heliosupine N-oxide, Heliosupin metabolite, inhibits muscarinic acetylcholine receptor (mAChR) with the IC50 of 350 μM. Heliosupine N-oxide is a pyrrolizidine alkaloid (PA) .
Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinity muscarinic receptor antagonist. Dexetimide can be used in studies of parkinson's disease .
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
Methacholine iodide is a potent muscarinic-3 (M3) agonist. Methacholine iodide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine iodide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine iodide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates .
Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects .
Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
VU6021625 is a selective antagonist muscarinic acetylcholine receptors (mAChRs), with the IC50 value of 0.44 nM, 57 nM for human M4 and rat M4, respectively .
Bencycloquidium bromide, a muscarinic M(3) receptor antagonist, is an anticholinergic compound that acts as an anticholinergic bronchodilator. Bencycloquidium bromide can be used in the study for rhinitis .
Racanisodamine is one of the racemic isomers of anisodamine, resembles anisodamine in pharmacological effect. Racanisodamine is a non-selective muscarinic antagonist, used as a component of eye drops for myopic control .
Tropatepine is an orally active, anticholinergicmuscarinic antagonist and can be used as an antiparkinsonian agent . Tropatepine is used to combat against extrapyramidal syndrome induced by neuroleptic agents .
VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC50 value of 155 nM. VU6004256 has the potential for the research of schizophrenia .
Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. [ 3H]Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors . Iperoxo is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist. Methacholine choride acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine choride shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine choride can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates .
Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates .
Dicyclomine (hydrochloride) (Standard) is the analytical standard of Dicyclomine (hydrochloride). This product is intended for research and analytical applications. Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively .
Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research .
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research .
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
(Rac)-Sabcomeline ((Rac)-SB-202026) serves as an M1/M4 muscarinic agonist, making it a valuable tool in the exploration of neurological disorders, including schizophrenia.
Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors .
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease .
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect[1].
Tazomeline is a selective M1 muscarinic receptor agonist. Tazomeline inhibits twitch height in rabbit vas deferens(IC50= 0.001 nM). Tazomeline can be used for research of neuropsychiatric disorders .
Homatropine (Bromide) (Standard) is the analytical standard of Homatropine (Bromide). This product is intended for research and analytical applications. Homatropine Bromide is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent .
Perlapine is a potent muscarinic DREADD (Designer Receptors Exclusively Activated by Designer agents) agonist Perlapine exhibits >10000-fold selectivity for hM3Dq over hM3 receptors .
Methacholine (chloride) (Standard) is the analytical standard of Methacholine (chloride). This product is intended for research and analytical applications. Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist. Methacholine choride acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine choride shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine choride can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates .
Aclidinium Bromide (LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist. Aclidinium Bromide has the potential for chronic obstructive pulmonary disease (COPD) research .
(±)-Darifenacin N-Oxide is the impurity of Darifenacin (HY-A0033). Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9 .
Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
Flavoxate-d4 (hydrochloride) (Rec-7-0040-d4) is the deuterium labeled Flavoxate hydrochloride. Flavoxate Hydrochloride is a muscarinic AChR antagonist used in various urinary syndromes and as an antispasmodic[1][2].
ONO 1603, a novel prolyl endopeptidase inhibitor investigated as a potential antidementia drug, demonstrated neuroprotective and neurotrophic effects in cerebellar granule cells similar to tetrahydroaminoacridine (THA). At a concentration of 0.03 microM, ONO 1603 promoted neuronal survival, enhanced neurite outgrowth, increased m3-muscarinic acetylcholine receptor (mAChR) mRNA levels, and stimulated mAChR-mediated signaling pathways. These findings suggest that ONO 1603 shares pharmacological similarities with THA, indicating its potential as a therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and neuronal function .
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Darifenacin-d4 is the deuterium labeled Darifenacin[1]. Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi)[2].
Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
Solifenacin-d7 (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Muscarine-d9 (iodide) is the deuterium labeled Muscarine iodide. Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist[1][2].
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Pteropodine (compound 3) is a monoterpenoid oxindole alkaloid that can be isolated from Hamelia patens. Pteropodine modulates the functions of M1 muscarinic and 5-HT2 receptors. Pteropodine has antioxidant and antimutagenic properties .
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.
MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research .
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration .
Atropine Oxide (Atropine oxidation) hydrochloride, a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings .
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
4-Hydroxy-1-(2-phenylethyl)piperidine is a building block that has been used in the synthesis of ligands of the muscarinic acetylcholine receptor (mAChR) or sigma non-opioid intracellular receptor 1 (σ1 receptor).
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
Baogongteng A ((-)-Bao Gong Teng A) is an optically active tropane alkaloid with hypotensive and miotic activity, and can be isolated from the Chinese herb Erycibe obtusifolia Benth. Baogongteng A is also a muscarinic agonist. Baogongteng A can be used for cardiovascular and glaucoma research .
Trihexyphenidyl (hydrochloride) (Standard) is the analytical standard of Trihexyphenidyl (hydrochloride). This product is intended for research and analytical applications. Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
ASP8302 is a positive allosteric modulator of muscarinic M3 Receptor. ASP8302 improves voiding efficiency and reduced residual urine volume in two voiding dysfunction models. ASP8302 can be used for research of underactive bladder .
Pancuronium dibromide, a bis-quaternary steroid, is a neuromuscular relaxant. Pancuronium dibromide inhibits neuromuscular transmission by competing with acetylcholine for binding sites on nACh receptors. Pancuronium dibromide also inhibits cardiac muscarinic receptors and has a sympathomimetic action .
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR(muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
Tiotropium (Bromide) (Standard) is the analytical standard of Tiotropium (Bromide). This product is intended for research and analytical applications. Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205)[1][2].
J 104129 fumarate is a selective and orally active muscarinic M3 antagonist with Ki values of 4.2 nM and 490 nM for M3 and M2, respectively. J 104129 fumarate antagonized ACh-induced bronchoconstriction. J 104129 fumarate has the potential for the research of obstructive airway disease .
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
Pirenzepine (LS 519 free base) is a selective M1 mAChR(muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
Tolterodine (tartrate) (Standard) is the analytical standard of Tolterodine (tartrate). This product is intended for research and analytical applications. Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant .
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB) .
Isopteropodine (Standard) is the analytical standard of Isopteropodine. This product is intended for research and analytical applications. Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors .
Solifenacin (Standard) is the analytical standard of Solifenacin. This product is intended for research and analytical applications. Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
CHF-6550 is an antagonist for muscarinic M3 receptor and an agonist for β2 adrenoceptor (MABA), with pKi of 9.3 and 10.6, respectively. CHF-6550 exhibits good hepatocyte clearance in rat models and good pharmacokinetic characteristics in guinea pigs .
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
Tropicamide (Standard) is the analytical standard of Tropicamide. This product is intended for research and analytical applications. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
Solifenacin (Succinate) (Standard) is the analytical standard of Solifenacin (Succinate). This product is intended for research and analytical applications. Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
(R,R)-Reboxetine mesylate is an antidepressant agent with great bioavailability. (R,R)-Reboxetine is the enantiomer of Reboxetine, which is a selective noradrenaline reuptake inhibitor. Reboxetine consists of (R,R) and (S,S) enantiomer, has low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals .
Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic .
β2AR/M-receptor agonist-1 (example 131) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-1 shows potency to β2 adrenoceptor with an EC50 value of 9.2 nM. β2AR/M-receptor agonist-1 also has potency to muscarinic receptor with a Ki value of 30.2 nM. β2AR/M-receptor agonist-1 shows MABA potency with an EC50 value of 4.0 nM .
Levophencynonate is a muscarinic receptor antagonist with anticholinergic activity. The biological activity of levophencynonate makes it a key target for the determination of its concentration in human plasma in medical research. Levophencynonate was analyzed by high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) and showed good specificity and linearity .
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
MIPS1455 is a light-activated M1 muscarinic acetylcholine receptor ligand with irreversible binding activity to the allosteric site of the receptor. MIPS1455 is a drug target under investigation for the suppression of cognitive deficits and may become a valuable molecular tool for further investigation of allosteric interactions of the receptor .
Levophencynonate is a muscarinic receptor antagonist with anticholinergic activity. The biological activity of levophencynonate makes it a key target for the determination of its concentration in human plasma in medical research. Levophencynonate was analyzed by high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) and showed good specificity and linearity .
(R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
Deschloroclozapine dihydrochloride, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [ 11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging .
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant .
Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [ 11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging .
SCH 57790 is a selective antegonist for muscarinic M2 receptor, which increases acetylcholine release, and thus improves cognitive performance. SCH 57790 reverses Scopolamine (HY-N0296)-induced memory deficits in mice, without significant toxicity (100 mg/kg).
Glycopyrrolate (Standard) is the analytical standard of Glycopyrrolate. This product is intended for research and analytical applications. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
Aclidinium (Bromide) (Standard) is the analytical standard of Aclidinium (Bromide). This product is intended for research and analytical applications. Aclidinium Bromide (LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist. Aclidinium Bromide has the potential for chronic obstructive pulmonary disease (COPD) research .
Tolterodine tartrate-d14 (Kabi-2234-d14) is deuterium labeled Tolterodine (tartrate). Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine .
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
Itameline (RU 47213) is a prodrug with oral and long-lasting cholinergic activity. Itameline is a novel tetrahydropyridine-oxime that is cleaved in vivo to form an active metabolite, RU 35963. RU 35963 is a muscarinic receptor agonist that is nonselective with respect to receptor subtypes. Itameline possesses the capacity to reduce memory deficits induced by an impairment of cholinergic transmission in the rat .
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively .
Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Xanomeline-d3 (LY-246708-d3) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
(±)-Epibatidine (CMI 545) dihydrochloride is an agonist of nicotinic with potent analgetic activity. (±)-Epibatidine (CMI 545) dihydrochloride is an alkaloid originally characterized from frog skin. (±)-Epibatidine (CMI 545) dihydrochloride have little or no activity at a variety of other central receptors, including opioid receptors, muscarinic receptors, adrenergic receptors, dopamine receptors, serotonin receptors, and gamma-aminobutyric acid receptors .
Pancuronium (dibromide) (Standard) is the analytical standard of Pancuronium (dibromide). This product is intended for research and analytical applications. Pancuronium dibromide, a bis-quaternary steroid, is a neuromuscular relaxant. Pancuronium dibromide inhibits neuromuscular transmission by competing with acetylcholine for binding sites on nACh receptors. Pancuronium dibromide also inhibits cardiac muscarinic receptors and has a sympathomimetic action .
(1R,3S-)Solifenacin-d5 (hydrochloride) is the deuterium labeled Solifenacin D5 hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively[1].
Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
5-Hydroxymethyl tolterodine (formate) (PNU-200577 (formic)) is an active metabolite of the muscarinic acetylcholine receptor antagonists Tolterodine (HY-A0024) and Fesoterodine (HY-70053). 5-Hydroxymethyl tolterodine (formate) is formed from tolterodine by the cytochrome P450 (CYP) isoform CYP2D6 and from fesoterodine by plasma esterases.
VU0029767 is an allosteric enhancer of the M1 muscarinic receptor with the activity to modulate M1 receptor activity. VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
Diphenidol is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea .
Arecoline (hydrobromide) (Standard) is the analytical standard of Arecoline (hydrobromide). This product is intended for research and analytical applications. Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia .
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with high affinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM) .
Atropine methyl (bromide) (Standard) is the analytical standard of Atropine methyl (bromide). This product is intended for research and analytical applications. Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine .
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
(E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models .
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR(muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia .
Ipratropium (bromide) (Standard) is the analytical standard of Ipratropium (bromide). This product is intended for research and analytical applications. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic,histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD) .
Ipratropium (bromide hydrate) (Standard) is the analytical standard of Ipratropium (bromide hydrate). This product is intended for research and analytical applications. Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Amitriptyline is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline also inhibits adrenergic, muscarinic,histamine and 5-HT receptors. Amitriptyline is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline has antidepressant activity .
Diphenidol (hydrochloride) (Standard) is the analytical standard of Diphenidol (hydrochloride). This product is intended for research and analytical applications. Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC50 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator .
Rociverine is an anticholinergic compound with smooth muscle relaxant activity. Rociverine showed different binding modes in five cloned muscarinic receptors. The cis stereoisomer of Rociverine showed a higher affinity change compared to the trans stereoisomer. The (1R,2R) configuration of Rociverine showed significantly higher affinity, even up to 240 times. The (1S,2S) configuration of Rociverine is very important for binding selectivity .
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects .
GS 283 is a compound with calcium antagonist and weak histamine and muscarinic receptor blocking activity, with activity in modulating contraction of guinea pig and rat tracheal smooth muscle. GS 283 inhibits contractions induced by carbachol, histamine (guinea pig only), and high H + in guinea pig and rat tracheal smooth muscle, inhibits Ca 2+-induced contractions in guinea pig tracheal smooth muscle, and at high concentrations completely abolishes contractions induced by carbachol in Ca 2+-free medium.
Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic,histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine maleate has antidepressive effects .
Olanzapine hydrochloride is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine hydrochloride is an atypical antipsychotic .
Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic,histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
Smilagenin (SMI) is a small-molecule steroidal sapogenin from Anemarrhena asphodeloides and Pelargonium hortorum widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases .
Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density .
Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD .
Quifenadine (Compound 3a), the hydroxyl-(diphenyl)methyl quinuclidine derivative, is a M3 receptor antagonist with an IC50 value > 1000 nM. Quifenadine can be used for the research of neurological disease .
BTM-1042 is a newly synthesized compound with antispasmodic effects. It can inhibit the twitch reaction of the guinea pig ileum under electrical stimulation and is not affected by naloxone. It has similar effects to atropine and can block muscarinic receptors, but has less effect on other types of receptors. BTM-1042 also has an inhibitory effect on the ileal reaction caused by nicotine and 5-hydroxytryptamine. BTM-1042 showed a dose-dependent inhibitory effect on the spontaneous movement of the rabbit stomach. In general, BTM-1042 is a agent with a strong antispasmodic effect.
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Nomifensine-d3 ((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects .
Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membrane tumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
Pimethixene maleate (Standard) is the analytical standard of Pimethixene maleate. This product is intended for research and analytical applications. Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
Anisodine hydrobromide is a neuroprotective compound that interacts with muscarinic receptors (M1-M5) in cerebral ischemic diseases. Anisodine hydrobromide effectively reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine hydrobromide demonstrates concentration-dependent inhibition of calcium ion influx and reactive oxygen species (ROS) levels, elucidating its neuroprotective mechanisms. Anisodine hydrobromide leads to decreased aspartate levels in HM cells during hypoxia, highlighting its effects on neurotransmitter modulation. Anisodine hydrobromide holds promising clinical prospects as a potential therapeutic agent for ischemic brain diseases, warranting further investigation into its mechanisms of action.
Arecaidine propargyl ester hydrobromide is an agonist of M2 muscarinic acetylcholine receptors and has the activity of inhibiting tumor cell proliferation. The application of arecaidine propargyl ester hydrobromide has shown that it can reduce the number of ovarian cancer cells in vitro and induce apoptosis and the production of reactive oxygen species (ROS) at specific concentrations. Arecaidine propargyl ester hydrobromide can also arrest cells at the G2/M phase of the cell cycle and increase the percentage of abnormal mitosis. Arecaidine propargyl ester hydrobromide is more sensitizing to ovarian surface epithelial cells with higher M2 receptor levels than to cancer cells. Arecaidine propargyl ester hydrobromide exhibits the effect of lowering arterial blood pressure when interacting with the cardiovascular system in a natural physiological state, indicating its potential pharmacological application .
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
β2AR/M-receptor agonist-2 (compound 15) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-2 shows potency to β2 adrenoceptor with an EC50 value of 3.7 nM. β2AR/M-receptor agonist-2 also has potency to human cloned M3 receptor with a Ki value of 0.73 nM. β2AR/M-receptor agonist-2 is a potent bronchodilator, it can be used for the research of chronic obstructive pulmonary disease (COPD) .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .
L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
L-Hyoscyamine (Standard) is the analytical standard of L-Hyoscyamine. This product is intended for research and analytical applications. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
(±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits α-adrenergic receptor activity. (±)-Scopolamine has Ki values of 33 μM and 7.25 nM for α1-adrenerg receptor and muscarinic cholinergic receptor, respectively .
L-Hyoscyamine (sulfate) (Standard) is the analytical standard of L-Hyoscyamine (sulfate). This product is intended for research and analytical applications. L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR .
Arecoline hydrochloride, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrochloride exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrochloride also can induce oxidative stress .
Arecoline, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress .
Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
Anisodamine (6-Hydroxyhyoscyamine), a belladonna alkaloid, is a non-subtype-selective muscarinic, and also a nicotinic cholinoceptor antagonist. Anisodamine employs in traditional Chinese medicine for many ailments, mainly to improve the microcirculation in states of shock, and also in organophosphate poisoning .
Anisodamine (hydrobromide) (Standard) is the analytical standard of Anisodamine (hydrobromide). This product is intended for research and analytical applications. Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .
Arecoline (hydrobromide) (Standard) is the analytical standard of Arecoline (hydrobromide). This product is intended for research and analytical applications. Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
Peimisine (Ebeiensine) hydrochloride is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine hydrochloride shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research .
Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research .
Scopolamine hydrochloride is a non-selective and high affinity (≤1 nM) muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. Scopolamine readily passes the blood brain barrier. Scopolamine also reversibly inhibits 5-HT3 receptor-responses with an IC50 of 2.09 μM . Scopolamine induces Alzheimer's disease-like pathology through alteration of cholinergic system .
Pilocarpine (Hydrochloride) (Standard) is the analytical standard of Pilocarpine (Hydrochloride). This product is intended for research and analytical applications. Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
Peimisine (Standard) is the analytical standard of Peimisine. This product is intended for research and analytical applications. Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research .
Pilocarpine (nitrate) (Standard) is the analytical standard of Pilocarpine (nitrate). This product is intended for research and analytical applications. Pilocarpine nitrate is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
Acetylcholine iodide is a muscarinic receptor modulator. Acetylcholine iodide specifically binds to muscarinic receptors, inhibits sodium absorption, and induces chloride secretion. Acetylcholine iodide changes intestinal ion transport, enhances intestinal secretory function, induces or maintains mammary gland development and lactation. Acetylcholine iodide can be used for intestinal ion transport regulation and mammary gland physiological function research .
Heliosupine N-oxide, Heliosupin metabolite, inhibits muscarinic acetylcholine receptor (mAChR) with the IC50 of 350 μM. Heliosupine N-oxide is a pyrrolizidine alkaloid (PA) .
Racanisodamine is one of the racemic isomers of anisodamine, resembles anisodamine in pharmacological effect. Racanisodamine is a non-selective muscarinic antagonist, used as a component of eye drops for myopic control .
Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors .
Pteropodine (compound 3) is a monoterpenoid oxindole alkaloid that can be isolated from Hamelia patens. Pteropodine modulates the functions of M1 muscarinic and 5-HT2 receptors. Pteropodine has antioxidant and antimutagenic properties .
Baogongteng A ((-)-Bao Gong Teng A) is an optically active tropane alkaloid with hypotensive and miotic activity, and can be isolated from the Chinese herb Erycibe obtusifolia Benth. Baogongteng A is also a muscarinic agonist. Baogongteng A can be used for cardiovascular and glaucoma research .
Trihexyphenidyl (hydrochloride) (Standard) is the analytical standard of Trihexyphenidyl (hydrochloride). This product is intended for research and analytical applications. Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research .
Isopteropodine (Standard) is the analytical standard of Isopteropodine. This product is intended for research and analytical applications. Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors .
(±)-Epibatidine (CMI 545) dihydrochloride is an agonist of nicotinic with potent analgetic activity. (±)-Epibatidine (CMI 545) dihydrochloride is an alkaloid originally characterized from frog skin. (±)-Epibatidine (CMI 545) dihydrochloride have little or no activity at a variety of other central receptors, including opioid receptors, muscarinic receptors, adrenergic receptors, dopamine receptors, serotonin receptors, and gamma-aminobutyric acid receptors .
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
Smilagenin (SMI) is a small-molecule steroidal sapogenin from Anemarrhena asphodeloides and Pelargonium hortorum widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases .
Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density .
Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD .
CHRM1, the muscarinic acetylcholine receptor, mediates cellular responses, including adenylate cyclase inhibition, phosphoinositide breakdown, and potassium channel modulation through G protein actions.It engages with GPRASP2 and TMEM147, contributing to a complex network of signaling pathways and cellular processes regulated by the receptor.CHRM1 Protein, Rat (His) is the recombinant rat-derived CHRM1 protein, expressed by E.coli , with N-6*His labeled tag.
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4].
Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride[1]. Tolterodine hydrochloride is a potent muscarinic receptor antagonist[2][3].
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect[1].
Flavoxate-d4 (hydrochloride) (Rec-7-0040-d4) is the deuterium labeled Flavoxate hydrochloride. Flavoxate Hydrochloride is a muscarinic AChR antagonist used in various urinary syndromes and as an antispasmodic[1][2].
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Darifenacin-d4 is the deuterium labeled Darifenacin[1]. Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi)[2].
Solifenacin-d7 (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Muscarine-d9 (iodide) is the deuterium labeled Muscarine iodide. Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist[1][2].
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205)[1][2].
Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases .
Tolterodine tartrate-d14 (Kabi-2234-d14) is deuterium labeled Tolterodine (tartrate). Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
Xanomeline-d3 (LY-246708-d3) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
(1R,3S-)Solifenacin-d5 (hydrochloride) is the deuterium labeled Solifenacin D5 hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively[1].
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR(muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Nomifensine-d3 ((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
Muscarinic Acetylcholine receptor M3 Antibody is an unconjugated, approximately 66 kDa, rabbit-derived, anti-Muscarinic Acetylcholine receptor M3 monoclonal antibody. Muscarinic Acetylcholine receptor M3 Antibody can be used for: WB expriments in human background without labeling.
Muscarinic Acetylcholine Receptor M2 Antibody (YA2610) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2610), targeting Muscarinic Acetylcholine Receptor M2, with a predicted molecular weight of 52 kDa (observed band size: 52 kDa). Muscarinic Acetylcholine Receptor M2 Antibody (YA2610) can be used for WB, IHC-P, IP experiment in human, mouse, rat background.
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
Arecaidine propargyl ester hydrobromide is an agonist of M2 muscarinic acetylcholine receptors and has the activity of inhibiting tumor cell proliferation. The application of arecaidine propargyl ester hydrobromide has shown that it can reduce the number of ovarian cancer cells in vitro and induce apoptosis and the production of reactive oxygen species (ROS) at specific concentrations. Arecaidine propargyl ester hydrobromide can also arrest cells at the G2/M phase of the cell cycle and increase the percentage of abnormal mitosis. Arecaidine propargyl ester hydrobromide is more sensitizing to ovarian surface epithelial cells with higher M2 receptor levels than to cancer cells. Arecaidine propargyl ester hydrobromide exhibits the effect of lowering arterial blood pressure when interacting with the cardiovascular system in a natural physiological state, indicating its potential pharmacological application .
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