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-170444
    ADS1017
    		Antagonist
    ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models.
    ADS1017
  • HY-113970
    Nebracetam
    		Agonist
    Nebracetam (WEB 1881 FU) is an orally active M1 muscarinic receptor agonist. Nebracetam can induce an increase in intracellular Ca2+ concentration, with an EC50 value of 1.59 mM. Nebracetam exhibits neuroprotective activity and the ability to improve cognitive impairment. Nebracetam can be used in the research of neurological diseases such as Alzheimer's disease.
    Nebracetam
  • HY-B1585A
    Caramiphen hydrochloride
    		Antagonist
    Caramiphen hydrochloride is a muscarinic antagonist. Caramiphen hydrochloride shows anticonvulsive properties. Caramiphen hydrochloride offers partial protection against Soman-induced seizures and neuropathology.
    Caramiphen hydrochloride
  • HY-124223
    AF-DX 384 methanesulfonate
    		Antagonist
    AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively). AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine.
    AF-DX 384 methanesulfonate
  • HY-182384
    VU6015241
    		Antagonist
    VU6015241 is a selective, blood-brain barrier-permeable M4 mAChR Antagonist with a Ki value of 43.3 nM. VU6015241 is used for the research of dystonia and related movement disorders.
    VU6015241
  • HY-A0002R
    Solifenacin Succinate (Standard)
    		Antagonist
    Solifenacin (Succinate) (Standard) is the analytical standard of Solifenacin (Succinate). This product is intended for research and analytical applications. Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
    Solifenacin Succinate (Standard)
  • HY-100795
    Pirmenol
    		Inhibitor 99.32%
    Pirmenol is an orally active antiarrhythmic agent. Pirmenol inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol can be used in the research of cardiovascular disease, such as atrial fibrillation.
    Pirmenol
  • HY-169814
    LU-25-077
    		Agonist
    Lu 25-077 is a brain-penetrant and pharmacologically active N-demethyl metabolite of Lu 25-109 (HY-101586), a partial M1 agonist and M2/M3 antagonist. Lu 25-077 can be utilized in neurological research.
    LU-25-077
  • HY-114743
    GS 283
    		Antagonist
    GS 283 is a compound with calcium antagonist and weak histamine and muscarinic receptor blocking activity, with activity in modulating contraction of guinea pig and rat tracheal smooth muscle. GS 283 inhibits contractions induced by carbachol, histamine (guinea pig only), and high H+ in guinea pig and rat tracheal smooth muscle, inhibits Ca2+-induced contractions in guinea pig tracheal smooth muscle, and at high concentrations completely abolishes contractions induced by carbachol in Ca2+-free medium.
    GS 283
  • HY-N0471S1
    L-Hyoscyamine-d3-1
    L-Hyoscyamine-d3-1 (Hyoscyamine-d3) is the deuterium labeled L-Hyoscyamine (HY-N0471). L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205).
    L-Hyoscyamine-d<sub>3</sub>-1
  • HY-137040A
    Tiemonium iodide
    		Antagonist
    Tiemonium iodide is a mAChR antagonist with antispasmodic properties. Tiemonium iodide can be used in nervous system research.
    Tiemonium iodide
  • HY-76570S1
    5-Hydroxymethyl Tolterodine-d14 formate
    		Antagonist
    5-Hydroxymethyl Tolterodine-d14 (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research.
    5-Hydroxymethyl Tolterodine-d<sub>14</sub> formate
  • HY-W008517R
    6-Hydroxytropinone (Standard)
    		Control
    6-Hydroxytropinone (Standard) is the analytical standard of 6-Hydroxytropinone. This product is intended for research and analytical applications. 6-Hydroxytropinone is a cyclic hydroxylation product of Tropinone (HY-Y0135), and serves as an indicator for tropane alkaloid metabolism in plants or microorganisms. 6-Hydroxytropinone itself has no significant anticholinergic toxicity, nor does it act as a substrate for Tropine (HY-N7061) dehydrogenase.
    6-Hydroxytropinone (Standard)
  • HY-W309130
    (S)-Tolterodine
    		Inhibitor
    (S)-Tolterodine is a muscarinic acetylcholine receptor (mAChR) inhibitor, with an IC50 of 588 nM.
    (S)-Tolterodine
  • HY-172339
    4-AcO-DALT hydrochloride
    		Inhibitor
    4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, histamine receptor 1 (H1), muscarinic M2 receptor and Sigma 2 receptor. 4-AcO-DALT hydrochloride shows Ki values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors.
    4-AcO-DALT hydrochloride
  • HY-76569S
    Desfesoterodine-d5
    		Antagonist
    Desfesoterodine-d5 (PNU-200577-d5) is the deuterium labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
    Desfesoterodine-d<sub>5</sub>
  • HY-14786
    Darotropium bromide
    		Antagonist
    Darotropium bromide (GSK233705), a long-acting muscarinic antagonist and an inhaled anticholinergic, can be used for the research of chronic obstructive pulmonary disease (COPD).
    Darotropium bromide
  • HY-118806
    AC-42
    		Agonist
    AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells.
    AC-42
  • HY-146102
    M1 ligand 1
    M1 ligand 1 (compound 3b-b) is a muscarinic acetylcholine receptor M1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer.
    M1 ligand 1
  • HY-G0021R
    N-Desmethylclozapine (Standard)
    		Agonist
    N-Desmethylclozapine (Standard) is the analytical standard of N-Desmethylclozapine. This product is intended for research and analytical applications. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine 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 is also a δ-opioid agonist.
    N-Desmethylclozapine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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