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-B1205B
    Atropine hydrobromide
    Antagonist
    Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia.
    Atropine hydrobromide
  • HY-13204B
    Biperiden lactate
    Inhibitor
    Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders.
    Biperiden lactate
  • HY-B0761
    (R,R)-Glycopyrrolate
    (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities.
    (R,R)-Glycopyrrolate
  • HY-P5846
    Muscarinic toxin 3
    Antagonist
    Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D2A2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity.
    Muscarinic toxin 3
  • HY-159177
    M4 mAChR Modulator-1
    Modulator
    M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment.
    M4 mAChR Modulator-1
  • HY-120329
    Lu 26-046
    Modulator
    Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats.
    Lu 26-046
  • 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-112076A
    Atropine methyl nitrate
    Antagonist
    Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, 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-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-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-17366R
    Clozapine N-oxide (Standard)
    Agonist
    Clozapine N-oxide (Standard) is the analytical standard of Clozapine N-oxide. This product is intended for research and analytical applications. Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier[1][2][3][4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].
    Clozapine N-oxide (Standard)
  • HY-100795
    Pirmenol
    Inhibitor
    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-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[1].
    5-Hydroxymethyl Tolterodine-d<sub>14</sub> formate
  • HY-W309130
    (S)-Tolterodine
    Inhibitor
    (S)-Tolterodine is a muscarinic acetylcholine receptor (mAChR) inhibitor, with an IC50 of 588 nM.
    (S)-Tolterodine
  • HY-B1277R
    Trihexyphenidyl (hydrochloride) (Standard)
    Antagonist
    Trihexyphenidyl (hydrochloride) (Standard) is the analytical standard of Trihexyphenidyl (hydrochloride). This product is intended for research and analytical applications. Trihexyphenidyl hydrochloride is a potent and selective M1 muscarinic receptor antagonist. Trihexyphenidyl hydrochloride shows anticholinergic activity, and can be used for Parkinson syndrome or dystonia research.
    Trihexyphenidyl (hydrochloride) (Standard)
  • 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
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