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-W010892R
    Scopolamine hydrobromide trihydrate (Standard)
    Antagonist
    Scopolamine hydrobromide trihydrate (Standard) is the analytical standard of Scopolamine hydrobromide trihydrate (HY-W010892). This product is intended for research and analytical applications. Scopolamine (Hyoscine) hydrobromide is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide can induce cognitive and memory deficits in animals. Scopolamine hydrobromide can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc.
    Scopolamine hydrobromide trihydrate (Standard)
  • HY-P1375A
    [D-Trp7,9,10]-Substance P TFA
    Inhibitor
    [D-Trp7,9,10]-Substance P TFA is a substance P analogue. Substance P stimulates substance P receptors but also inhibits ion conductance through nicotinic acetylcholine receptors.
    [D-Trp7,9,10]-Substance P TFA
  • HY-13204S2
    rel-Biperiden EP impurity A-d5
    Inhibitor
    rel-Biperiden EP impurity A-d5 is deuterium labeled Biperiden (hydrochloride).
    rel-Biperiden EP impurity A-d<sub>5</sub>
  • HY-N0471C
    L-Hyoscyamine sulfate hydrate
    Antagonist
    L-Hyoscyamine sulfate hydrate, a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate hydrate is a levo-isomer to Atropine (HY-B1205).
    L-Hyoscyamine sulfate hydrate
  • HY-171981
    VU6002703
    Modulator
    VU6002703 (Compound 17) is a BBB-penetrable M4 mAChR positive allosteric modulator (PAM) with an EC50 of 0.6  μM for hM4. VU6002703 can be used for neuropsychiatric and rare genetic CNS disorders research.
    VU6002703
  • HY-135329
    Solifenacin D5 hydrochloride
    Antagonist
    Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
    Solifenacin D5 hydrochloride
  • HY-117966
    Bibn 140
    Bibn 140 is a pyridine derivative substituted with a benzene ring, which has high affinity (Ki: 12 nM) and selectivity for M2 mAChR receptors over M1 receptors.
    Bibn 140
  • HY-B1296S1
    Promethazine-d4
    Antagonist
    Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties.
    Promethazine-d<sub>4</sub>
  • HY-107650
    Milameline hydrochloride
    Agonist
    Milameline (CI 979; RU35926) hydrochloride is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydrochloride has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydrochloride has a higher affinity for sites [3H]CMD (IC50 = 20 nM), than [3H]QNB, (IC50 = 3059 nM). Milameline hydrochloride produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydrochloride can be used for the study of Alzheimer’s Disease.
    Milameline hydrochloride
  • HY-U00079B
    (S)-Vamicamide
    Antagonist
    (S)-Vamicamide ((S)-FK-176) is an anticholinergic compound.
    (S)-Vamicamide
  • HY-A0033S1
    Darifenacin-d4
    Darifenacin-d4 is the deuterium labeled Darifenacin. Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi).
    Darifenacin-d<sub>4</sub>
  • HY-100154
    Darenzepine
    Inhibitor
    Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.
    Darenzepine
  • HY-121470
    Vesamicol
    Vesamicol is a compound used to synthesize radiolabeled derivatives that can be used as sigma receptor ligands for tumor targeting inhibition and have shown certain potential in cellular uptake, biodistribution and inhibition experiments.
    Vesamicol
  • HY-17037S1
    Pirenzepine-d8 dihydrochloride
    Antagonist
    Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). 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-d<sub>8</sub> dihydrochloride
  • HY-149732
    M1/M4 muscarinic agonist 3
    Agonist
    M1/M4 muscarinic agonist 3 (compound 44) is a muscarinic mAChR M1/M4 agonist with EC50s of 31 nM and 9.3 nM, respectively.
    M1/M4 muscarinic agonist 3
  • HY-B1388R
    Homatropine methylbromide (Standard)
    Antagonist
    Homatropine (methylbromide) (Standard) is the analytical standard of Homatropine (methylbromide). This product is intended for research and analytical applications.
    Homatropine methylbromide (Standard)
  • HY-U00079A
    Vamicamide
    Antagonist
    Vamicamide (FK-176) is an orally active competitive mAChR antagonist that inhibits contractions induced by cholinergic nerve stimulation by preventing mAChR agonists from binding to mAChR. Vamicamide exhibits a good anti-bladder spasm effect, with a pA2 value of 6.82 in bladder tissue. Vamicamide can be used in research within the field of neurological diseases.
    Vamicamide
  • HY-113692
    AZD-9164 bromide
    Antagonist
    AZD-9164 (bromide) is a long-acting muscarinic M3 antagonist. AZD-9164 (bromide) is promising for research of airways diseases, such as chronic obstructive pulmonary disease (COPD) or asthma.
    AZD-9164 bromide
  • HY-148961
    HTL-9936
    Agonist
    HTL-9936 is a selective M1 muscarinic acetylcholine receptor (M1-mAChR) agonist. HTL-9936 is promising for research of neurodegenerative disorders (e.g., Alzheimer’s).
    HTL-9936
  • HY-149702
    M1/M4 muscarinic agonist 1
    Agonist
    M1/M4 muscarinic agonist 1 (compound 41) is a selective muscarinic M4/M1 agonist with EC50 values of 14 and 55 nM for M4 and M1, respectively. M1/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusional disorder, etc.
    M1/M4 muscarinic agonist 1
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