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-B1205A
    Atropine sulfate
    Antagonist 99.63%
    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.
    Atropine sulfate
  • HY-107647
    (S)-(+)-Dimethindene maleate
    Antagonist 99.80%
    (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48).
    (S)-(+)-Dimethindene maleate
  • HY-13410
    Xanomeline oxalate
    Agonist 99.93%
    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.
    Xanomeline oxalate
  • HY-B0527
    Amitriptyline
    Inhibitor 99.94%
    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.
    Amitriptyline
  • HY-B0489
    Arecoline hydrobromide
    Agonist 99.95%
    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.
    Arecoline hydrobromide
  • HY-B0520A
    Benztropine mesylate
    Inhibitor 99.85%
    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
    Benztropine mesylate
  • HY-122743
    Iperoxo
    Agonist 99.48%
    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. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors when labeled with tritium.
    Iperoxo
  • HY-132812
    Emraclidine
    Modulator 99.82%
    Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases.
    Emraclidine
  • HY-17360
    Tiotropium Bromide
    Antagonist 99.91%
    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 Bromide
  • HY-17465
    Glycopyrrolate
    Antagonist 99.93%
    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.
    Glycopyrrolate
  • HY-100958
    4-DAMP
    Antagonist 99.96%
    4-DAMP (4-DAMP methiodide) is a potent and selective antagonist of M3 receptors and also has a high affinity for the closely-related M5 receptors. 4-DAMP combined with 5-Fluorouracil (5-Fu) (HY-90006) could significantly reduce the cell viability and enhance apoptosis in MKN45 and BGC823 gastric cancer cells. 4-DAMP inhibits lipopolysaccharide (LPS)- and tobacco-induced pulmonary inflammation and reduces mucin 5AC (MUC5AC), oligomeric mucus/gel-forming secretion.
    4-DAMP
  • HY-101372A
    Oxotremorine M iodide
    Agonist ≥98.0%
    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.
    Oxotremorine M iodide
  • HY-100234
    DREADD agonist 21
    Agonist 99.46%
    DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
    DREADD agonist 21
  • HY-B0781
    Promethazine hydrochloride
    Antagonist 99.20%
    Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
    Promethazine hydrochloride
  • HY-101239
    Oxotremorine sesquifumarate
    Agonist ≥98.0%
    Oxotremorine sesquifumarate is a mAChR agonist that mainly activates M2 receptors. Oxotremorine sesquifumarate can be used for neurological research.
    Oxotremorine sesquifumarate
  • HY-B0499A
    Otilonium bromide
    Inhibitor 99.69%
    Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome.
    Otilonium bromide
  • HY-A0016
    Dronedarone
    Inhibitor 99.93%
    Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
    Dronedarone
  • HY-17037
    Pirenzepine dihydrochloride
    Antagonist 99.84%
    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.
    Pirenzepine dihydrochloride
  • HY-B1223
    Anethole trithione
    Agonist 99.54%
    Anethole trithione, a sulfur heterocyclic choleretic, is a bile secretion-stimulating agent. Anethole trithione enhances salivary secretion and increases mAChRs, and can be used for dry mouth research.
    Anethole trithione
  • HY-B0461
    Trospium chloride
    Antagonist 99.93%
    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
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