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-A0139
    Thiothixene
    Antagonist
    Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    Thiothixene
  • 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-B0416R
    Gallamine Triethiodide (Standard)
    Inhibitor
    Gallamine Triethiodide (Standard) is the analytical standard of Gallamine Triethiodide. This product is intended for research and analytical applications. Gallamine Triethiodide is a cholinergic receptor inhibitor and non-depolarizing blocker with an IC50 of 68.0±8.4 μM.
    Gallamine Triethiodide (Standard)
  • HY-B0547AR
    Homatropine (Bromide) (Standard)
    Antagonist
    Homatropine (Bromide) (Standard) is the analytical standard of Homatropine (Bromide). This product is intended for research and analytical applications. Homatropine Bromide is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent.
    Homatropine (Bromide) (Standard)
  • HY-129709
    DAC 5945
    Antagonist
    DAC 5945 is a potent muscarinic antagonist in the airways than in the heart, with pKi values of 8.3 and 7.52 for M1 and M2, respectively.
    DAC 5945
  • HY-B0499AR
    Otilonium (bromide) (Standard)
    Inhibitor
    Otilonium (bromide) (Standard) is the analytical standard of Otilonium (bromide). This product is intended for research and analytical applications. Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome.
    Otilonium (bromide) (Standard)
  • HY-134004R
    Pentoxyverine (Standard)
    Antagonist
    Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
    Pentoxyverine (Standard)
  • HY-121168
    Aprophen
    Inhibitor
    Aprophen (Aprofene) is an antimuscarinic inhibitor. Aprophen can be used for the research of central nervous system.
    Aprophen
  • HY-N0471R
    L-Hyoscyamine (Standard)
    Antagonist
    L-Hyoscyamine (Standard) is the analytical standard of L-Hyoscyamine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0662R
    Imidafenacin (Standard)
    Inhibitor
    Imidafenacin (Standard) is the analytical standard of Imidafenacin. This product is intended for research and analytical applications. Imidafenacin (KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors.
    Imidafenacin (Standard)
  • HY-B1621
    Cyclopentolate
    Antagonist
    Cyclopentolate (DL-Cyclopentolate) is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate is an anti-muscarinic agent commonly used in the ophthalmologic practice.
    Cyclopentolate
  • HY-W700319
    (Rac)-5-Carboxy tolterodine
    Control
    (Rac)-5-Carboxy tolterodine is an inactive metabolite of the muscarinic acetylcholine receptor antagonist Tolterodine (HY-A0024).
    (Rac)-5-Carboxy tolterodine
  • HY-B0327A
    Irsogladine maleate
    Inhibitor
    Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.
    Irsogladine maleate
  • HY-B0267CS
    (R)-Oxybutynin-d10
    Antagonist
    (R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction.
    (R)-Oxybutynin-d<sub>10</sub>
  • HY-A0016R
    Dronedarone (Standard)
    Inhibitor
    Dronedarone (Standard) is the analytical standard of Dronedarone. This product is intended for research and analytical applications. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
    Dronedarone (Standard)
  • HY-13204AS
    Biperiden-d5
    Inhibitor
    Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders.
    Biperiden-d<sub>5</sub>
  • HY-14144R
    Aclidinium (Bromide) (Standard)
    Antagonist
    Aclidinium (Bromide) (Standard) is the analytical standard of Aclidinium (Bromide). This product is intended for research and analytical applications. Aclidinium Bromide (LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist. Aclidinium Bromide has the potential for chronic obstructive pulmonary disease (COPD) research.
    Aclidinium (Bromide) (Standard)
  • HY-115413
    LG50643
    Antagonist
    LG50643 is a potent and selective M3 muscarinic receptor antagonist (pKi=8.64).
    LG50643
  • HY-B0781R
    Promethazine (hydrochloride) (Standard)
    Antagonist
    Promethazine (hydrochloride) (Standard) is the analytical standard of Promethazine (hydrochloride). This product is intended for research and analytical applications. Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
    Promethazine (hydrochloride) (Standard)
  • HY-76569B
    5-Hydroxymethyl tolterodine formate
    Antagonist
    5-Hydroxymethyl tolterodine (formate) (PNU-200577 (formic)) is an active metabolite of the muscarinic acetylcholine receptor antagonists Tolterodine (HY-A0024) and Fesoterodine (HY-70053). 5-Hydroxymethyl tolterodine (formate) is formed from tolterodine by the cytochrome P450 (CYP) isoform CYP2D6 and from fesoterodine by plasma esterases.
    5-Hydroxymethyl tolterodine formate
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