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-137976
    Penehyclidine hydrochloride
    		Antagonist 99.2%
    Penehyclidine (Penequinine) hydrochloride, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.
    Penehyclidine hydrochloride
  • HY-128855
    Talsaclidine
    		Agonist 98.75%
    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.
    Talsaclidine
  • HY-B0962A
    Piperidolate
    		Antagonist 99.34%
    Piperidolate is a cholinergic antagonist. Piperidolate prevents ventricular fibrillation during hypothermic cardiac manipulations to support cardiac procedures post-preoperative defibrillation. Piperidolate causes dose-dependent cardiac depression. Piperidolate can be used for the research of ventricular fibrillation.
    Piperidolate
  • HY-B0520
    Benztropine
    		Inhibitor 98.12%
    Benztropine (Benzatropine; Benzotropine) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
    Benztropine
  • HY-100336
    AC260584
    		Agonist 99.48%
    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
    AC260584
  • HY-14825A
    Tarafenacin D-tartrate
    		Antagonist 99.86%
    Tarafenacin (SVT-40776) D-tartrate is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin D-tartrate does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin D-tartrate can be used in the research of overactive bladder.
    Tarafenacin D-tartrate
  • 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-107654
    Muscarine iodide
    		Agonist 99.55%
    Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist.
    Muscarine iodide
  • HY-121806
    VU0486846
    		Modulator 99.5%
    VU0486846 is an orally active and selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) .
    VU0486846
  • HY-116480
    LY593093
    		Agonist 98.82%
    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.
    LY593093
  • HY-B0461R
    Trospium chloride (Standard)
    		Antagonist
    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.
    Trospium chloride (Standard)
  • HY-N1433
    Phytolaccagenin
    		Activator 99.86%
    Phytolaccagenin is a triterpenoid saponin aglycone, Antifungal agent, vasodilator, antihypertensive agent, and anti-inflammatory agent. Phytolaccagenin activates vascular and cardiac Muscarinic receptors, blocks cardiac β-adrenergic receptors, and inhibits voltage-dependent calcium channels in blood vessels. Phytolaccagenin inhibits the growth of Candida albicans and Cryptococcus neoformans. Phytolaccagenin induces vasodilation, produces negative inotropic and negative chronotropic effects, reduces mean arterial pressure, and inhibits LPS-induced inflammation. Phytolaccagenin exhibits enhanced antihypertensive effects in high salt-induced hypertensive rats. Phytolaccagenin can be used in the research of candidiasis, cryptococcosis, hypertension, and inflammation-related diseases.
    Phytolaccagenin
  • HY-B1475
    Anisotropine bromide
    		Antagonist 98.0%
    Anisotropine (Octatropine) bromide is an orally active anticholinergic muscarinic antagonist. Anisotropine bromide can inhibit gastric acid secretion and is used as an adjunct to peptic ulcers.
    Anisotropine bromide
  • HY-105545
    Dexetimide
    		Antagonist 99.94%
    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.
    Dexetimide
  • HY-70020
    Cevimeline
    		Agonist 99.88%
    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).
    Cevimeline
  • HY-14541S
    Olanzapine-d3
    		Antagonist 99.78%
    Olanzapine-d3 (LY170053-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.
    Olanzapine-d<sub>3</sub>
  • 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 99.93%
    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-107649
    Zamifenacin fumarate
    		Antagonist 99.0%
    Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
    Zamifenacin fumarate
  • HY-120184
    VU0467485
    		Agonist 99.29%
    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.
    VU0467485
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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