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-17037AR
    Pirenzepine (Standard)
    		Antagonist
    Pirenzepine (Standard) is the analytical standard of Pirenzepine. This product is intended for research and analytical applications. Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells.
    Pirenzepine (Standard)
  • HY-B0267C
    (R)-Oxybutynin
    		Antagonist
    (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
  • HY-151198
    CHF-6366
    		Antagonist
    CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD).
    CHF-6366
  • HY-B0406AR
    Bethanechol chloride (Standard)
    		Agonist
    Bethanechol (chloride) (Standard) is the analytical standard of Bethanechol (chloride). This product is intended for research and analytical applications. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
    Bethanechol chloride (Standard)
  • HY-B0489A
    Arecoline hydrochloride
    		Agonist
    Arecoline hydrochloride, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrochloride exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrochloride also can induce oxidative stress.
    Arecoline hydrochloride
  • HY-128584
    VU6005806
    		Agonist
    VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
    VU6005806
  • HY-160440A
    VU6021625
    		Antagonist
    VU6021625 is a selective antagonist muscarinic acetylcholine receptors (mAChRs), with the IC50 value of 0.44 nM, 57 nM for human M4 and rat M4, respectively.
    VU6021625
  • HY-14560A
    (R,R)-Reboxetine mesylate
    (R,R)-Reboxetine mesylate is an antidepressant agent with great bioavailability. (R,R)-Reboxetine is the enantiomer of Reboxetine, which is a selective noradrenaline reuptake inhibitor. Reboxetine consists of (R,R) and (S,S) enantiomer, has low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals.
    (R,R)-Reboxetine mesylate
  • HY-142119
    Penehyclidine
    		Antagonist
    Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.
    Penehyclidine
  • HY-76570S
    (Rac)-5-Hydroxymethyl Tolterodine-d14
    		Antagonist
    (Rac)-5-Hydroxymethyl Tolterodine-d14 is the 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.
    (Rac)-5-Hydroxymethyl Tolterodine-d<sub>14</sub>
  • HY-17360S
    Tiotropium-d3 bromide
    		Antagonist
    Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
    Tiotropium-d<sub>3</sub> bromide
  • HY-171843
    TD-6301
    		Antagonist
    TD-6301 is a bladder-selective M2/4 muscarinic receptor antagonist. TD-6301 binds to and blocks M2/4 muscarinic receptors with high selectivity, especially human M2 receptors with strong affinity (Ki = 0.36 nM). TD-6301 inhibits volume-induced bladder contractions (ID50 = 0.075 mg/kg). TD-6301 can be used in the research of overactive bladder.
    TD-6301
  • HY-B0480A
    Brompheniramine
    		Inhibitor
    Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine 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 has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
    Brompheniramine
  • HY-W011040
    LY320135
    		Modulator
    LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
    LY320135
  • HY-12980A
    Batefenterol Succinate
    		Antagonist
    Batefenterol Succinate (GSK961081 Succinate) is a first-of-its-kind inhaled bifunctional bronchodilator with smooth muscle relaxant properties. The activities of Batefenterol Succinate include acting as a smooth muscle parasympathetic antagonist and a beta2-adrenoceptor agonist. Batefenterol Succinate is used to improve respiratory function, especially in patients with chronic obstructive pulmonary disease (COPD).
    Batefenterol Succinate
  • HY-169178
    VU6016235
    		Inhibitor
    VU6016235 is a highly selective, orally available, positive allosteric modulator of the M4 mAChR with in vivo inhibitory potency in animal models of psychosis..
    VU6016235
  • HY-B1789
    Telenzepine
    		Antagonist
    Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM).
    Telenzepine
  • HY-W010892R
    Scopolamine hydrobromide trihydrate (Standard)
    		Antagonist
    Scopolamine hydrobromide trihydrate (Standard) is the analytical standard of Scopolamine hydrobromide trihydrate (HY-W010892). This product is intended for research and analytical applications. Scopolamine (Hyoscine) hydrobromide is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrobromide can induce cognitive and memory deficits in animals. Scopolamine hydrobromide can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc.
    Scopolamine hydrobromide trihydrate (Standard)
  • HY-P1375A
    [D-Trp7,9,10]-Substance P TFA
    		Inhibitor
    [D-Trp7,9,10]-Substance P TFA is a substance P analogue. Substance P stimulates substance P receptors but also inhibits ion conductance through nicotinic acetylcholine receptors.
    [D-Trp7,9,10]-Substance P TFA
  • HY-13204S2
    rel-Biperiden EP impurity A-d5
    		Inhibitor
    rel-Biperiden EP impurity A-d5 is deuterium labeled Biperiden (hydrochloride).
    rel-Biperiden EP impurity A-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity
mAChR Isoform Comparison

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