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-119918
    Cycrimine
    		Antagonist 99.85%
    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.
    Cycrimine
  • HY-B1388
    Homatropine methylbromide
    		Antagonist 98.0%
    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.
    Homatropine methylbromide
  • HY-P0102
    Dipeptide diaminobutyroyl benzylamide diacetate
    		Antagonist 99.63%
    Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a mAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate can induce muscle relaxation. Dipeptide diaminobutyroyl benzylamide diacetate can be used in the research of skin aging, especially facial wrinkles (such as crow's feet and wrinkles around the eyes).
    Dipeptide diaminobutyroyl benzylamide diacetate
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    		Antagonist
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline hydrochloride (Standard)
  • HY-160888
    ASP8302
    		Modulator 98.95%
    ASP8302 is a positive and allosteric muscarinic M3 receptor modulator. ASP8302 improves voiding efficiency and reduced residual urine volume in two voiding dysfunction models. ASP8302 can be used for research of underactive bladder.
    ASP8302
  • HY-107651
    VU 0365114
    		Agonist 99.41%
    VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells.
    VU 0365114
  • HY-N7004
    Arborine
    		Inhibitor 99.77%
    Arborine inhibits the peripheral action of acetylcholine and induces a fall in blood pressure.
    Arborine
  • HY-101839
    ML381
    		Antagonist 99.87%
    ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies.
    ML381
  • HY-B0480
    Brompheniramine maleate
    		Inhibitor 99.78%
    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
  • HY-14562
    TBPB
    		Agonist 99.74%
    TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC50=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis).
    TBPB
  • HY-121027
    Anagyrine
    		Antagonist 98.15%
    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
  • HY-101281
    VU 6008667
    		Inhibitor 99.53%
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
    VU 6008667
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride
    		Antagonist 99.65%
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d<sub>6</sub> hydrochloride
  • HY-B0962A
    Piperidolate
    		Inhibitor 99.71%
    Piperidolate is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
    Piperidolate
  • HY-100336
    AC260584
    		Agonist 99.48%
    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
    AC260584
  • HY-100795A
    Pirmenol hydrochloride
    		Inhibitor 99.34%
    Pirmenol ((±)-Pirmenol) hydrochloride is an orally active antiarrhythmic agent. Pirmenol hydrochloride inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol hydrochloride can be used in the research of cardiovascular disease, such as atrial fibrillation.
    Pirmenol hydrochloride
  • HY-131891
    JHU37152
    		Agonist 99.45%
    JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.
    JHU37152
  • HY-111130
    Methapyrilene
    		Antagonist 99.66%
    Methapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats.
    Methapyrilene
  • HY-101036
    Choline bitartrate
    		98.0%
    Choline bitartrate is a vitamin-like essential nutrient, can affect diseases such as liver disease, atherosclerosis and neurological disorders. Choline bitartrate is a precursor for the neurotransmitter acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.
    Choline bitartrate
  • HY-107654
    Muscarine iodide
    		Agonist
    Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist.
    Muscarine iodide
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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