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-B1277A
    Trihexyphenidyl
    		Antagonist
    Trihexyphenidyl is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research.
    Trihexyphenidyl
  • HY-B0489R
    Arecoline hydrobromide (Standard)
    		Agonist
    Arecoline (hydrobromide) (Standard) is the analytical standard of Arecoline (hydrobromide). This product is intended for research and analytical applications. 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 (Standard)
  • HY-115871A
    (Rac)-PDE4-IN-4
    		Antagonist
    (Rac)-PDE4-IN-4 is the diastereomer mixture of PDE4-IN-4 (HY-115871). PDE4-IN-4 is a dual M3 (pIC50 = 10.2) antagonist-PDE4 (pIC50 = 8.8) inhibitor for the inhaled research of pulmonary diseases.
    (Rac)-PDE4-IN-4
  • HY-105545C
    Dexetimide hydrochloride
    		Antagonist
    Dexetimide hydrochloride ((+)-Benzetimide hydrochloride) is an antimuscarinic drug with the activity of suppressing neuroleptic-induced Parkinson's syndrome. Dexetimide hydrochloride is used to improve the symptoms of movement disorders caused by the use of neuroleptics. Dexetimide hydrochloride, as the (-)-enantiomer of (-)-Benzetimide, shows the ability to selectively inhibit cholinergic receptors.
    Dexetimide hydrochloride
  • HY-139126
    (±)-Muscarine chloride
    		Agonist
    (±)-Muscarine chloride is the racemate of Muscarine chloride. Muscarine is a prototype muscarinic acetylcholine receptor agonist.
    (±)-Muscarine chloride
  • HY-14539B
    Clozapine dihydrochloride
    		Modulator
    Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine dihydrochloride
  • HY-43711
    Nor-benzetimide
    		Antagonist
    Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.
    Nor-benzetimide
  • HY-156128
    Imidafenacin Metabolite M4
    Imidafenacin Metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist Imidafenacin (HY-B0662).
    Imidafenacin Metabolite M4
  • HY-108340
    PF-06767832
    		Agonist
    PF-06767832 is a potent muscarinic M1 selective positive allosteric modulator (PAM), with the EC50 of 60 nM. PF-06767832 has good brain penetration.
    PF-06767832
  • 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-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[1].
    (±)-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
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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