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-106949
    Tazomeline
    Agonist
    Tazomeline is a selective M1 muscarinic receptor agonist. Tazomeline inhibits twitch height in rabbit vas deferens(IC50= 0.001 nM). Tazomeline can be used for research of neuropsychiatric disorders.
    Tazomeline
  • HY-119082
    (E/Z)-VU0029767
    Modulator
    (E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
    (E/Z)-VU0029767
  • HY-105771
    Parapenzolate bromide
    Antagonist
    Parapenzolate bromide, an antispasmodic, is an orally active mAChR antagonist. Parapenzolate bromide is an anticholinergic agent.
    Parapenzolate bromide
  • HY-162491
    JR-6
    Agonist
    JR-6 is a Gi/o pathway biased and muscarinic M2 selective partial agonist.
    JR-6
  • HY-B0321R
    Tropicamide (Standard)
    Antagonist
    Tropicamide (Standard) is the analytical standard of Tropicamide. This product is intended for research and analytical applications. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops.
    Tropicamide (Standard)
  • HY-76570S2
    (Rac)-5-hydroxymethyl Tolterodine-d5
    Antagonist
    (Rac)-5-hydroxymethyl Tolterodine-d5 ((Rac)-Desfesoterodine-d5; (Rac)-PNU-200577-d5) is deuterium-labeled (Rac)-5-Hydroxymethyl Tolterodine (HY-76570).
    (Rac)-5-hydroxymethyl Tolterodine-d5
  • HY-G0021S1
    N-Desmethylclozapine-d8 hydrochloride
    Agonist 99.74%
    N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
    N-Desmethylclozapine-d<sub>8</sub> hydrochloride
  • HY-120322
    MK-0969
    Antagonist
    MK-0969 is a M3 antagonist. MK-0969 can be used for research about chronic obstructive pulmonary disease and urinary incontinence.
    MK-0969
  • HY-109006
    Ilmetropium iodide
    Inhibitor
    Ilmetropium iodide is an anticholinergic agent. Ilmetropium iodide selectively blocks M-cholinergic receptors of bronchial muscle, reduces or prevents bronchoconstrictor response associated with both cholinergic stimulation, as well as the impact of the factors that provoke bronchospasm. Strength and selectivity of ilmetropium iodide action substantially exceeds Atropine sulfate (HY-B1205A) and Ipratropium bromide (HY-B0241).
    Ilmetropium iodide
  • HY-116586A
    (Rac)-AF710B
    Agonist
    (Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.
    (Rac)-AF710B
  • HY-B0520AR
    Benztropine (mesylate) (Standard)
    Inhibitor
    Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
    Benztropine (mesylate) (Standard)
  • HY-17037S
    Pirenzepine-d8
    Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
    Pirenzepine-d<sub>8</sub>
  • HY-107656
    PTAC oxalate
    Modulator
    PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects.
    PTAC oxalate
  • HY-122086
    Prifinium bromide
    Inhibitor
    Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect.
    Prifinium bromide
  • HY-B1339AS
    Dicyclomine-d4
    Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
    Dicyclomine-d<sub>4</sub>
  • HY-105435
    FR121196
    FR121196 is a cognitive enhancer, and ameliorates Scopolamine (HY-N0296)-induced memory deficit. FR121196 is an antidementia compound.
    FR121196
  • HY-155819
    M3/PDE4 modulator-1
    Antagonist
    M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model.
    M3/PDE4 modulator-1
  • HY-N0214A
    Peimisine hydrochloride
    Antagonist
    Peimisine (Ebeiensine) hydrochloride is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine hydrochloride shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research.
    Peimisine hydrochloride
  • HY-22437S1
    (±)-Darifenacin-d4 hydrobromide
    Antagonist
    (±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
    (±)-Darifenacin-d<sub>4</sub> hydrobromide
  • HY-W014208
    NGX-267
    Agonist
    NGX-267 is a selective agonist of the actin M1 receptor, which has high selectivity among the five actin receptor subtypes, especially for the M1 receptor rather than the M3 receptor. NGX-267 also has significant differences in affinity for dopamine D2 and 5-HT2B receptors.
    NGX-267
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