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

mAChR

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 Related Products (166):

Cat. No. Product Name Effect Purity
  • HY-17366
    Clozapine N-oxide Agonist 99.98%
    Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
  • HY-42110
    Deschloroclozapine Agonist 99.79%
    Deschloroclozapine is a potent, high affinity, selective, metabolically stable agonist of muscarinic-based DREADDs. Deschloroclozapine inhibites [3H]quinuclidinyl benzilate (QNB) binding to hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM. Deschloroclozapine is reported with utility in both mice and non-human primates for a variety of applications.
  • HY-B0726
    Pilocarpine Hydrochloride Agonist ≥98.0%
    Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
  • HY-14539
    Clozapine Agonist 99.74%
    Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
  • HY-B1205
    Atropine Antagonist ≥98.0%
    Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist, with anti-myopia effect. Atropine blocks the inhibitory effect of ACh on heart rate and contractility, potentially also leading to tachyarrhythmias.
  • HY-109013
    Sofpironium bromide Inhibitor
    Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.
  • HY-14825
    Tarafenacin Antagonist
    Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
  • HY-139044
    VU6000918 Activator
    VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4.
  • HY-14541
    Olanzapine Antagonist 99.89%
    Olanzapine (LY170053) is a selective 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 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
  • HY-17366A
    Clozapine N-oxide dihydrochloride Agonist 98.17%
    Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
  • HY-B0527A
    Amitriptyline hydrochloride Inhibitor 99.56%
    Amitriptyline hydrochloride 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 hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
  • HY-B0106
    Levetiracetam Inhibitor 99.99%
    Levetiracetam (UCB L059) is a selective M2 muscarinic acetylcholine receptors (mAChR) inhibitor. Antiepileptic agent.
  • HY-A0012
    Darifenacin hydrobromide Antagonist 98.28%
    Darifenacin hydrobromide (UK-88525 hydrobromide) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
  • HY-A0083
    Methacholine chloride Agonist ≥98.0%
    Methacholine (Acetyl-β-methylcholine) chloride acts a muscarinic M3 receptor agonist in the parasympathetic nervous system. Methacholine chloride acts directly on acetylcholine receptors on smooth muscle causing contraction and airway narrowing. Methacholine challenges are widely used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
  • HY-B0499A
    Otilonium bromide Inhibitor 99.48%
    Octylonium bromide (SP63) is an antimuscarinic used as a spasmolytic agent.
  • HY-B0394
    Atropine sulfate monohydrate Antagonist ≥98.0%
    Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.
  • HY-112209
    VU0467154 Agonist ≥98.0%
    VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
  • HY-B1188
    Propantheline bromide Inhibitor
    Propantheline bromide is an antimuscarinic agent, used for the treatment of hyperhidrosis, cramps or spasms of the stomach, intestines or bladder, and enuresis.
  • HY-N0214
    Peimisine Antagonist 99.51%
    Peimisine (Ebeiensine) non-competitively antagonizes tracheal smooth muscle muscarinic M receptor and inhibits smooth muscle contraction caused by Ach. Peimisine excits β-receptor, restrains the release of internal calcium, and promotes to releaseing NO in order to relax tracheal smooth muscle and relieve asthma.
  • HY-N0471
    L-Hyoscyamine Antagonist 99.32%
    L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205).
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