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-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-176710
    PAD-PF2
    Antagonist 99.94%
    PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer.
    PAD-PF2
  • HY-119918
    Cycrimine
    Antagonist 99.85%
    Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder.
    Cycrimine
  • HY-101841
    LY 2033298
    Activator 99.87%
    LY 2033298 is a selective positive allosteric modulator of the muscarinic M4 receptor. LY 2033298 can be used in the study of psychiatric disorders.
    LY 2033298
  • 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-B1806A
    Tridihexethyl chloride
    Antagonist
    Tridihexethyl (Pathilon) chloride is an orally active anticholinergic agent and mAChR antagonist, shows activities of antimuscarinic and anticholinergic. Tridihexethyl chloride shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. Tridihexethyl chloride can be used in studies of peptic ulcer disease and acquired nystagmus .
    Tridihexethyl chloride
  • HY-112076A
    Atropine methyl nitrate
    Antagonist 99.77%
    Atropine methyl bromide (Methylatropine nitrate), an antagonist of muscarinic acetylcholine receptors (mAChR), is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine.
    Atropine methyl nitrate
  • HY-123337
    Zamifenacin
    Antagonist 99.24%
    Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
    Zamifenacin
  • HY-108340
    PF-06767832
    Agonist 98.37%
    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-U00082
    Tigloidin
    Antagonist 98.39%
    Tigloidin is an analogue of atropine, with anticholinergic activity.
    Tigloidin
  • HY-157956
    LASSBio-873
    Agonist 99.82%
    LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine.
    LASSBio-873
  • HY-14539A
    Clozapine hydrochloride
    Modulator 99.83%
    Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine hydrochloride
  • HY-16171
    Diphenmanil methylsulfate
    Antagonist 99.83%
    Diphemanil methylsulfate is a quaternary ammonium anticholinergic.
    Diphenmanil methylsulfate
  • HY-B1132
    Clidinium bromide
    Antagonist 99.42%
    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-116490
    Guvacoline hydrobromide
    Agonist 99.01%
    Guvacoline hydrobromide, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal mAChR.
    Guvacoline hydrobromide
  • HY-176200
    VU6008055
    Activator 99.43%
    VU6008055 (AF98943) is a brain-penetrant, orally active and selective muscarinic acetylcholine receptor subtype 4 (mAChR4) activator with human EC50 values of 73.4 nM. VU6008055 potentiates mAChR4 receptor activity in the presence of acetylcholine, and exhibits no activity at mAChR1, mAChR3, or mAChR5. VU6008055 can be used for the research of schizophrenia, parkinson’s disease, alzheimer’s disease.
    VU6008055
  • HY-13340
    VU0152100
    Modulator 98.98%
    VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia.
    VU0152100
  • 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-B0480A
    Brompheniramine
    Inhibitor 99.82%
    Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
    Brompheniramine
  • HY-N4157
    Isopteropodine
    Activator 99.13%
    Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research.
    Isopteropodine
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