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-43711
    Nor-benzetimide
    Antagonist
    Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.
    Nor-benzetimide
  • HY-186083
    Propylbenzilylcholine mustard
    Antagonist
    Propylbenzilylcholine mustard (PrBCM) is an irreversible, covalently binding selective antagonist targeting rat cardiac muscarinic receptors, with a preference for muscarinic receptor subtypes that show low affinity for agonists. Propylbenzilylcholine mustard inactivates such receptors in a dose- and time-dependent manner in vitro, and its receptor selectivity remains stable across different ionic strengths and in GTP-containing buffer systems. Propylbenzilylcholine mustard can be applied to basic pharmacological studies on the structure and function of muscarinic receptors, especially focusing on the heterogeneity of cardiac muscarinic receptors and related cardiovascular pharmacological research.
    Propylbenzilylcholine mustard
  • HY-117284A
    Eucatropine hydrochloride
    Inhibitor
    Eucatropine hydrochloride is a potent muscarinic acetylcholine receptor (mAChR) inhibitor with an IC50 value of 0.583 μM. Eucatropine hydrochloride acts as an anticholinergic agent. Eucatropine hydrochloride produces behavioral effects via central cholinergic receptive sites in cats.
    Eucatropine hydrochloride
  • HY-156128
    Imidafenacin Metabolite M4
    Imidafenacin Metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist Imidafenacin (HY-B0662).
    Imidafenacin Metabolite M4
  • HY-108157
    A-72055
    Agonist
    A-72055 is a partial agonist of muscarinic receptors. A-72055 has binding activity to both M1 and M2 receptors, with Ki values of 32 nM and 30 nM, respectively. A-72055 can enhance cognitive function and improve learning and memory deficits. A-72055 has better security. A-72055 can be used for research on neurological disorders such as cognitive impairment.
    A-72055
  • HY-W710400
    Quifenadine-d10
    Quifenadine-d10 is the deuterium labeled Quifenadine (HY-122761). Quifenadine (Compound 3a), the hydroxyl-(diphenyl)methyl quinuclidine derivative, is a M3 receptor antagonist with an IC50 value > 1000 nM. Quifenadine can be used for the research of neurological disease.
    Quifenadine-d<sub>10</sub>
  • HY-19092
    YM-796 dihydroxybutanedioate
    Agonist
    YM-796 dihydroxybutanedioate is a selective muscarinic M1 receptor agonist. YM-796 dihydroxybutanedioate can improve cognitive impairment and reduce amyloid plaque deposition. YM-796 dihydroxybutanedioate can be used in the research of cognitive impairment diseases such as Alzheimer's disease.
    YM-796 dihydroxybutanedioate
  • HY-B1055R
    Pentoxyverine citrate (Standard)
    Antagonist
    Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[4].
    Pentoxyverine citrate (Standard)
  • HY-22437S
    (±)-Darifenacin-d4
    Antagonist
    (±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist.
    (±)-Darifenacin-d<sub>4</sub>
  • HY-12100S1
    Umeclidinium-d10 bromide
    Antagonist
    Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
    Umeclidinium-d<sub>10</sub> bromide
  • HY-107644
    AQ-RA 741
    Antagonist
    AQ-RA 741 is a potent and selective M 2 antagonist. AQ-RA 741 inhibits the vagally or agonist-induced bradycardia in rats, cats and guinea-pigs. AQ-RA 741 is used in bradycardiac disorders research.
    AQ-RA 741
  • HY-B1487A
    Procyclidine
    Antagonist
    Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
    Procyclidine
  • HY-148525
    PF-4348235
    Antagonist
    β2AR/M-receptor agonist-2 (compound 15) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-2 shows potency to β2 adrenoceptor with an EC50 value of 3.7 nM. β2AR/M-receptor agonist-2 also has potency to human cloned M3 receptor with a Ki value of 0.73 nM. β2AR/M-receptor agonist-2 is a potent bronchodilator, it can be used for the research of chronic obstructive pulmonary disease (COPD).
    PF-4348235
  • HY-U00001
    Phenglutarimid
    Inhibitor
    Phenglutarimid is an anticholinergic used as an antiparkinsonian agent.
    Phenglutarimid
  • HY-101653
    MHP 133
    Inhibitor
    MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
    MHP 133
  • HY-120802
    Navafenterol
    Antagonist
    Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
    Navafenterol
  • HY-149704
    M1/M2/M4 muscarinic agonist 1
    Agonist
    M1/M2/M4 muscarinic agonist 1 (Compound 42) is a muscarinic M4/M1/M2 agonist with EC50 values of 6.5, 26 and 210 nM for M4/M1/M2, respectively. M1/M2/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusion, etc.
    M1/M2/M4 muscarinic agonist 1
  • HY-A0016S
    Dronedarone-d6 hydrochloride
    Inhibitor
    Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride 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 hydrochloride is a substrate for and a moderate inhibitor of CYP3A4.
    Dronedarone-d<sub>6</sub> hydrochloride
  • HY-B1689A
    Methantheline bromide
    Methantheline bromide is a quaternary Ammonium derivate with anticholinergic activity. Methantheline bromide results in a significant greater reduction of axillary sweat production. Methyl bromide can be used in the research of intractable peptic ulcers.
    Methantheline bromide
  • HY-131196
    M3 mAChR agonist 1
    Agonist
    M3 mAChR agonist 1 is an M3-preferring M3/M5 mAChR dual positive allosteric modulators (PAM). M3 mAChR agonist 1 shows excellent subtype selectivity over other subtypes of mAChRs including M1, M2, and M4 mAChRs. M3 mAChR agonist 1 increases the contraction of isolated rat bladder strips by modulating the M3 muscarinic acetylcholine receptor, leading to enhanced signaling pathways. M3 mAChR agonist 1 can be used for the research of endocrinology.
    M3 mAChR agonist 1
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