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-B0480R
    Brompheniramine maleate (Standard)
    		Inhibitor
    Brompheniramine (maleate) (Standard) is the analytical standard of Brompheniramine (maleate). This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate 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 maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
    Brompheniramine maleate (Standard)
  • HY-167849
    Sofpironium tosylate
    		Inhibitor
    Sofpironium (BBI 4000) tosylate is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium tosylate reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium tosylate also has a high afnity for the M1, M2, M4 and M5 subtypes.
    Sofpironium tosylate
  • HY-120792
    DAU 5884
    		Antagonist
    DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
    DAU 5884
  • HY-B1277S
    Trihexyphenidyl-d5 hydrochloride
    		Inhibitor
    Trihexyphenidyl-d5 (hydrochloride) is deuterium labeled Trihexyphenidyl (hydrochloride).
    Trihexyphenidyl-d<sub>5</sub> hydrochloride
  • HY-B1339S
    Dicyclomine-d4 hydrochloride
    Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride 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. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo.
    Dicyclomine-d<sub>4</sub> hydrochloride
  • HY-173031
    KTX-005
    		Agonist
    KTX-005 is the agonist for mAChR that regulates the signaling pathway of the neurotransmitter acetylcholine, and can be used for research of schizophrenia.
    KTX-005
  • HY-15502
    PF-3635659
    		Antagonist
    PF-3635659 is a potent antagonist of the muscarinic M3 receptor (mAChR3). PF-3635659 can be used for chronic obstructive pulmonary disease (COPD) research.
    PF-3635659
  • HY-B0241S1
    Ipratropium-d7 bromide
    		Antagonist
    Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
    Ipratropium-d<sub>7</sub> bromide
  • HY-19752
    VU0357017
    		Agonist
    VU0357017 (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 can be used for the research of Alzheimer’s disease and schizophrenia.
    VU0357017
  • HY-120842
    RLH-033
    RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [3H](+)-pentazocine with a Ki of 50 pM.
    RLH-033
  • HY-17037R
    Pirenzepine dihydrochloride (Standard)
    		Antagonist
    Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells.
    Pirenzepine dihydrochloride (Standard)
  • HY-126862
    AQ-RA 721
    		Antagonist
    AQ-RA 721 is a muscarinic receptor antagonist with differential affinity for the m4 and M2 sites, which can be used to characterize muscarinic receptor subtypes. Other muscarinic receptor antagonists have differential affinity for the M1 (rat cerebral cortex), M2 (rat heart), M3 (rat submandibular gland), m4 (receptor expressed in Chinese hamster ovary cells transfected with CHO), and guinea pig uterine smooth muscle at the muscarinic binding site.
    AQ-RA 721
  • HY-106432
    Sabcomeline
    		Agonist
    Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research.
    Sabcomeline
  • HY-116459
    trans-Cevimeline hydrochloride
    		Agonist
    Trans-Cevimeline (AF102A) (hydrochloride), as a trans-isomer of AF102B, is a M1 selective cholinergic agonist. Trans-Cevimeline (AF102A) (hydrochloride) can be used for the research of Alzheimer's disease.
    trans-Cevimeline hydrochloride
  • HY-A0083R
    Methacholine chloride (Standard)
    		Agonist
    Methacholine (chloride) (Standard) is the analytical standard of Methacholine (chloride). This product is intended for research and analytical applications. Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist. Methacholine choride acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine choride shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine choride can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
    Methacholine chloride (Standard)
  • HY-B1006R
    Pilocarpine nitrate (Standard)
    		Agonist
    Pilocarpine (nitrate) (Standard) is the analytical standard of Pilocarpine (nitrate). This product is intended for research and analytical applications. Pilocarpine nitrate is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
    Pilocarpine nitrate (Standard)
  • HY-134971
    AE9C90CB
    		Antagonist
    AE9C90CB, muscarinic receptor antagonist, has greater affinity for M3 muscarinic receptors with pKi of 9.90 and was 20-fold more selective for M3 than for M2 muscarinic receptors.
    AE9C90CB
  • HY-14541S1
    Olanzapine-d4
    		Antagonist
    Olanzapine-d4 (LY170053-d4) is deuterium-labeled Olanzapine (HY-14541).
    Olanzapine-d<sub>4</sub>
  • HY-B0241R
    Ipratropium bromide (Standard)
    		Antagonist
    Ipratropium (bromide) (Standard) is the analytical standard of Ipratropium (bromide). This product is intended for research and analytical applications. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma.
    Ipratropium bromide (Standard)
  • HY-76772R
    Cevimeline hydrochloride hemihydrate (Standard)
    		Agonist
    Cevimeline (hydrochloride hemihydrate) (Standard) is the analytical standard of Cevimeline (hydrochloride hemihydrate). This product is intended for research and analytical applications. Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
    Cevimeline hydrochloride hemihydrate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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