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-147028
    M4 mAChR agonist-1
    		Agonist 98.95%
    M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC50 >10 μM for human M4.
    M4 mAChR agonist-1
  • HY-101839
    ML381
    		Antagonist 99.87%
    ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies.
    ML381
  • HY-B1475
    Anisotropine bromide
    		Antagonist 98.0%
    Anisotropine (Octatropine) bromide is an orally active anticholinergic muscarinic antagonist. Anisotropine bromide can inhibit gastric acid secretion and is used as an adjunct to peptic ulcers.
    Anisotropine bromide
  • HY-105545
    Dexetimide
    		Antagonist 99.94%
    Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinity muscarinic receptor antagonist. Dexetimide can be used in studies of parkinson's disease.
    Dexetimide
  • HY-14562
    TBPB
    		Agonist 99.74%
    TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC50=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis).
    TBPB
  • HY-121027
    Anagyrine
    		Antagonist 98.15%
    Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR.
    Anagyrine
  • HY-B1132
    Clidinium bromide
    		Antagonist 99.0%
    Clidinium bromide is a quaternary amine antimuscarinic agent. Clidinium bromide may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines in vivo.
    Clidinium bromide
  • HY-14541S
    Olanzapine-d3
    		Antagonist 99.09%
    Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active 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 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>3</sub>
  • HY-101281
    VU 6008667
    		Inhibitor 99.53%
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
    VU 6008667
  • HY-139044
    VU6000918
    		Activator 99.92%
    VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4.
    VU6000918
  • HY-173396
    VU0467319
    		Modulator 98.53%
    VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC50: 492 nM). VU0467319 is selective (EC50 > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research.
    VU0467319
  • HY-120184
    VU0467485
    		Agonist 99.29%
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
    VU0467485
  • HY-14541R
    Olanzapine (Standard)
    		Antagonist
    Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active 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.
    Olanzapine (Standard)
  • HY-100336
    AC260584
    		Agonist 99.48%
    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
    AC260584
  • HY-122203A
    PCS1055
    		Antagonist 98.02%
    PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively.
    PCS1055
  • HY-107655
    Arecaidine but-2-ynyl ester tosylate
    		Agonist 99.95%
    Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research. Arecaidine but-2-ynyl ester (tosylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Arecaidine but-2-ynyl ester tosylate
  • HY-P1376A
    G-Protein antagonist peptide TFA
    		Inhibitor
    G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
    G-Protein antagonist peptide TFA
  • HY-123337
    Zamifenacin
    		Antagonist 99.81%
    Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
    Zamifenacin
  • HY-121806
    VU0486846
    		Modulator 99.5%
    VU0486846 is an orally active and selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) .
    VU0486846
  • HY-116480
    LY593093
    		Agonist 98.82%
    LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC50 of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research.
    LY593093
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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