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

mAChR

Muscarinic acetylcholine receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-A0033
    Darifenacin
    Antagonist 99.81%
    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.
    Darifenacin
  • HY-120081A
    Metixene hydrochloride hydrate
    Antagonist 99.92%
    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 hydrochloride hydrate
  • HY-B1339
    Dicyclomine hydrochloride
    Inhibitor ≥98.0%
    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.
    Dicyclomine hydrochloride
  • HY-76570
    (Rac)-5-Hydroxymethyl Tolterodine
    Antagonist 99.59%
    (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)-5-Hydroxymethyl Tolterodine
  • HY-B0416
    Gallamine Triethiodide
    Inhibitor ≥98.0%
    Gallamine Triethiodide is a cholinergic receptor inhibitor and non-depolarizing blocker with an IC50 of 68.0±8.4 μM.
    Gallamine Triethiodide
  • HY-B0549A
    Flavoxate hydrochloride
    Antagonist 99.85%
    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.
    Flavoxate hydrochloride
  • HY-N0584
    Anisodamine
    Antagonist 99.02%
    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
  • HY-G0021
    N-Desmethylclozapine
    Agonist 98.99%
    N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
    N-Desmethylclozapine
  • HY-B1789A
    Telenzepine dihydrochloride
    Antagonist 99.08%
    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.
    Telenzepine dihydrochloride
  • HY-17037A
    Pirenzepine
    Antagonist 99.02%
    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.
    Pirenzepine
  • HY-101381
    Otenzepad
    Antagonist 99.93%
    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.
    Otenzepad
  • HY-101086
    Acetylcholine iodide
    98.59%
    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.
    Acetylcholine iodide
  • HY-12157
    VU 0238429
    Agonist 99.96%
    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
    VU 0238429
  • HY-13204A
    Biperiden
    Inhibitor 99.74%
    Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic 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.
    Biperiden
  • HY-15618
    MK-7622
    Modulator 99.89%
    MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
    MK-7622
  • HY-12158
    VU0238441
    Activator 99.88%
    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.
    VU0238441
  • HY-B0344
    Methscopolamine bromide
    Inhibitor 99.81%
    Methscopolamine Bromide is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Methscopolamine bromide
  • HY-B0267A
    Oxybutynin chloride
    Antagonist 99.15%
    Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB). Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Oxybutynin chloride
  • HY-19752A
    VU0357017 hydrochloride
    Agonist 99.91%
    VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic 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.
    VU0357017 hydrochloride
  • HY-32067
    Aceclidine
    Modulator 99.23%
    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
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