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.
mAChR Isoform Specific Products
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mAChR Inhibitors
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mAChR Agonists
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mAChR Antagonists
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mAChR Activators
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mAChR Modulators
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mAChR Inducer
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mAChR Controls
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mAChR Ligands
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mAChR Related Products (727)
Related Products (727)
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Antibodies (2)
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mAChR Isoform Comparison
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LG50643
0 ImagesCat. No.: HY-115413CAS No.: 111372-42-0LG50643 is a potent and selective M3 muscarinic receptor antagonist (pKi=8.64).
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VU6035406
0 ImagesCat. No.: HY-184883CAS No.: 2746405-41-2VU6035406 is a functionally selective mAChR inhibitor, with mAChR IC50 values of 21 nM, 51 nM and 47 nM against human, rat and mouse targets, respectively. VU6035406 does not act as a P-glycoprotein substrate. VU6035406 shows extremely low inhibitory activity against cytochrome P450 1A2, 2C9, 2D6 and 3A4. VU6035406 can be used in the research of neurological and psychiatric disorders.
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Benzetimide hydrochloride (Standard)
0 ImagesSynonyms: R4929 (Standard); Dioxatrine (Standard)Benzetimide hydrochloride (Standard) (R4929 (Standard); Dioxatrine (Standard)) is the analytical standard of Benzetimide hydrochloride (HY-B1547A). This product is intended for research and analytical applications. Benzetimide hydrochloride (R4929) is a blood-brain barrier-permeable muscarinic acetylcholine receptor antagonist. Benzetimide hydrochloride blocks cholinergic receptor sites. Benzetimide hydrochloride induces mydriasis, prevents acetylcholine-induced muscle contraction, inhibits pilocarpine (HY-B0726A)-induced parasympathomimetic effects, and exhibits antisecretory activity. Benzetimide hydrochloride can be used in research related to Parkinson's disease.
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Tolterodine tartrate-d14
0 ImagesCat. No.: HY-90010SCAS No.: 1191280-48-4Synonyms: Kabi-2234-d14; PNU-200583E-d14Tolterodine tartrate-d14 (Kabi-2234-d14) is deuterium labeled Tolterodine tartrate. Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder.
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(S)-(+)-Dimethindene maleate (Standard)
0 ImagesCat. No.: HY-107647RCAS No.: 136152-65-3(S)-(+)-Dimethindene maleate (Standard) is the analytical standard of (S)-(+)-Dimethindene (maleate) (HY-107647). This product is intended for research and analytical applications. (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48).
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Promethazine hydrochloride (Standard)
0 ImagesPromethazine (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.
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5-Hydroxymethyl tolterodine formate
0 ImagesCat. No.: HY-76569BCAS No.: 380636-49-7Synonyms: PNU-200577 formic5-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.
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Revefenacin (Standard)
0 ImagesCat. No.: HY-15851RCAS No.: 864750-70-9Synonyms: TD-4208 (Standard); GSK1160724 (Standard)Revefenacin (Standard) is the analytical standard of Revefenacin. This product is intended for research and analytical applications. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
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Alvameline maleate
0 ImagesCat. No.: HY-101586ACAS No.: 219581-36-9Synonyms: Lu 25-109 maleateAlvameline (Lu 25-109) maleate is a partial agonist of M1 and an antagonist of M2/M3. Alvameline maleate competitively antagonizes contractions induced by ammonium chloride (HY-Y1269) and electrical field stimulation in human detrusor muscle, indicating its potential application in regulating bladder function. Additionally, alvameline maleate can improve cognitive function following traumatic brain injury in rats.
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Sabcomeline hydrochloride (Standard)
0 ImagesCat. No.: HY-106432ARCAS No.: 159912-58-0Synonyms: SB-202026 hydrochloride (Standard); Memric hydrochloride (Standard)Sabcomeline hydrochloride (Standard) is the analytical standard of Sabcomeline hydrochloride (HY-106432A). This product is intended for research and analytical applications. Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research.
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Umeclidinium bromide (Standard)
0 ImagesCat. No.: HY-12100RCAS No.: 869113-09-7Synonyms: GSK573719A (Standard)Umeclidinium (bromide) (Standard) is the analytical standard of Umeclidinium (bromide). This product is intended for research and analytical applications. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
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Arecaidine-propargyl ester
0 ImagesCat. No.: HY-183853CAS No.: 35516-99-5Arecaidine-propargyl ester is a selective M2 muscarinic receptor agonist with blood-brain barrier permeability, with a pKi of 5.91 for hm1, 7.06 for hm2, 6.07 for hm3, 6.01 for hm4, and 6.03 for hm5. Arecaidine-propargyl ester stimulates central and peripheral muscarinic receptors. Arecaidine-propargyl ester increases intracellular ROS, induces DNA damage and Apoptosis, and upregulates the expression of MnSOD and SIRT1. Arecaidine-propargyl ester reduces sympathetic nerve outflow, induces dose-dependent hypotension, and triggers negative chronotropic effects at high peripheral doses. Arecaidine-propargyl ester can be used in research related to Alzheimer's disease and glioblastoma.
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Scotanamine D
0 ImagesCat. No.: HY-N12302CAS No.: 1698873-84-5Synonyms: N1-Dihydrocaffeoyl, N10-caffeoyl spermidineScotanamine D (N1-Dihydrocaffeoyl, N10-caffeoyl spermidine) is a spermidine alkaloid. It can be isolated from S. tangutica. Scotanamine D potently and selectively inhibits the activity of the M1 muscarinic acetylcholine receptor, with an IC50 of 32 nM. It can be used in studies related to Parkinson's disease.
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Deschloroclozapine (Standard)
0 ImagesDeschloroclozapine (Standard) is the analytical standard of Deschloroclozapine (HY-42110). This product is intended for research and analytical applications. Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.
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Dronedarone-d6
0 ImagesCat. No.: HY-A0016S3CAS No.: 1132693-87-8Synonyms: SR 33589-d6Dronedarone-d6 (SR 33589-d6) is deuterium labeled Dronedarone. 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.
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Oxotremorine M iodide (Standard)
0 ImagesOxotremorine M (iodide) (Standard) is the analytical standard of Oxotremorine M (iodide) (HY-101372A). This product is intended for research and analytical applications. Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.
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Atropine methyl bromide (Standard)
0 ImagesCat. No.: HY-112076RCAS No.: 2870-71-5Synonyms: Methylatropine bromide (Standard)Atropine methyl bromide (Standard) is the analytical standard of Atropine methyl bromide. This product is intended for research and analytical applications. Atropine methyl bromide (Methylatropine bromide), an antagonist of muscarinic acetylcholine receptors (mAChR), 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.
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Piroheptine
0 ImagesCat. No.: HY-W683866CAS No.: 16378-21-5Piroheptine is a muscarinic acetylcholine receptor (mAChR) antagonist and dopamine reuptake inhibitor. Piroheptine blocks the high-affinity dopamine transport system, prevents MPP+ uptake into dopaminergic neurons, and exerts anticholinergic activity. Piroheptine completely prevents MPTP (HY-W114750)-induced loss of striatal dopamine and DOPAC, and increases striatal dopamine levels. Piroheptine can be used in studies related to Parkinson's disease.
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Ethopropazine hydrochloride (Standard)
0 ImagesSynonyms: Isothazine (Standard)Ethopropazine (hydrochloride) (Standard) is the analytical standard of Ethopropazine (hydrochloride) (HY-107922). This product is intended for research and analytical applications. Ethopropazine (Isothazine) hydrochloride is a potent and selective BChE inhibitor, a poor AChE inhibitor and a non-selective mAChR and NMDA antagonist. Ethopropazine hydrochloride has anticholinergic, antihistamine, antiadrenergic actions and properties. Ethopropazine hydrochloride alleviates thermal hyperalgesia in a dose dependent manner. Ethopropazine hydrochloride can be used for the research of Parkinson’s disease.
