2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mAChR

mAChR

Muscarinic acetylcholine receptor

mAChR

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mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia.

mAChR Isoform Specific Products:

mAChR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107654S
    Muscarine-d9 iodide
    		Agonist
    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].
    Muscarine-d<sub>9</sub> iodide
  • HY-148533
    β2AR agonist /M-receptor antagonist-1
    		Antagonist
    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).
    β2AR agonist /M-receptor antagonist-1
  • HY-B0726S1
    Pilocarpine-d5 hydrochloride
    		Agonist
    Pilocarpine-d5 hydrochloride is deuterated labeled Pilocarpine hydrochloride (HY-B0726). Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
    Pilocarpine-d<sub>5</sub> hydrochloride
  • HY-120682
    UH-AH 37
    		Antagonist
    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.
    UH-AH 37
  • HY-B0547
    Homatropine
    		Antagonist
    Homatropine is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent.
    Homatropine
  • HY-162662
    VU6008677
    		Modulator
    VU6008677 is a positive allosteric modulator (PAM) for M4, with EC50 of 120 nM for hM4. VU6008677 inhibits cytochrome P450, exhibits good pharmacokinetic characteristics in rats.
    VU6008677
  • HY-106564A
    Flutropium bromide
    		Inhibitor
    Flutropium bromide (Ba 598Br) is a organic bromide salt of flutropium. Flutropium bromide shows an anticholinergic effect. Flutropium bromide effectively suppresses spasms and it can be used for the research of asthma and chronic obstructive pulmonary disease.
    Flutropium bromide
  • HY-163702
    CHF-6550
    		Antagonist
    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.
    CHF-6550
  • HY-B0549
    Flavoxate
    		Antagonist
    Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR 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.
    Flavoxate
  • HY-101197
    SM-21 maleate
    SM 21 maleate, 2-phenoxyalkanoic acid ester, binds to central muscarinic recrptor with affinity of 0.174 μM.
    SM-21 maleate
  • HY-A0012R
    Darifenacin (hydrobromide) (Standard)
    		Antagonist
    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.
    Darifenacin (hydrobromide) (Standard)
  • HY-W909173
    TAAR1 agonist 2
    		Agonist
    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.
    TAAR1 agonist 2
  • HY-N4080
    Cyclobuxine D
    		Inhibitor
    Cyclobuxine D is a steroidal alkaloid extracted from Buxus microphylla. Cyclobuxine D has a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and Ba++−induced contraction of the longitudinal muscle isolated from the rabbit jejunum.
    Cyclobuxine D
  • HY-A0024S
    Tolterodine-d14 hydrochloride
    		≥99.0%
    Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride[1]. Tolterodine hydrochloride is a potent muscarinic receptor antagonist[2][3].
    Tolterodine-d<sub>14</sub> hydrochloride
  • HY-120802A
    Navafenterol saccharinate
    		Antagonist
    Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
    Navafenterol saccharinate
  • HY-B0549AS
    Flavoxate-d4 hydrochloride
    		Antagonist
    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].
    Flavoxate-d<sub>4</sub> hydrochloride
  • HY-13204S1
    rel-Biperiden-d5
    		Inhibitor
    rel-Biperiden-d5 is deuterium labeled Biperiden (hydrochloride).
    rel-Biperiden-d<sub>5</sub>
  • HY-159829
    Direclidine
    		Agonist
    Direclidine is a muscarinic M4 receptor positive allosteric modulator.
    Direclidine
  • HY-B0480R
    Brompheniramine (maleate) (Standard)
    		Inhibitor
    Brompheniramine (maleate) (Standard) is the analytical standard of Brompheniramine (maleate). This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
    Brompheniramine (maleate) (Standard)
  • HY-167849
    Sofpironium tosylate
    		Inhibitor
    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.
    Sofpironium tosylate
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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