mAChR
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.
Targets for mAChR
Products for mAChR
- Cat.No. Product Name Information
- GC34957 (+)-Cevimeline hydrochloride hemihydrate (+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
- GC11219 (R)-(+)-Tolterodine (R)-(+)-Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.
- GC63452 (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).
- GC30859 AC260584 AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
- GC64332 Aceclidine Aceclidine is a modulator of M3 muscarinic acetylcholine receptor.
- GC14096 Aclidinium Bromide LAMAs antagonist
- GC10219 AF-DX 116 AF-DX 116 (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
- GC30996 Alvameline (Lu 25-109) Alvameline (Lu 25-109) (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
- GC31815 Ambutonium bromide (BL700) Ambutonium bromide (BL700) is an acetylcholine antagonist.
- GC60049 Anisodamine hydrobromide Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist.
- GC35381 Arborine Arborine inhibits the peripheral action of acetylcholine and induces a fall in blood pressure.
- GC10264 Arecoline hydrobromide muscarinic acetylcholine receptor agonist
- GC16526 Atropine MAChRs antagonist
- GC35427 Atropine methyl bromide A muscarinic acetylcholine receptor antagonist
- GC35428 Atropine sulfate Atropine (Tropine tropate) sulfate 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.
- GC63827 Atropine sulfate monohydrate Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.
- GC31690 Batefenterol (GSK961081) Batefenterol (GSK961081) (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
- GC35492 Benzamide Derivative 1 Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18.
- GC30925 Benzetimide hydrochloride (R4929) Benzetimide hydrochloride (R4929) is a muscarinic acetylcholine receptor antagonist.
- GC16791 Benztropine mesylate Dopamine transporter (DAT) inhibitor
- GC31942 Beperidium iodide (SX 810) Beperidium iodide (SX 810) shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
- GC14419 Bethanechol chloride Muscarinic receptor agonist
- GC35524 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.
- GC10621 Biperiden HCl Biperiden (KL 373) hydrochloride 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.
- GC15758 BQCA positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR)
- GC32039 BTM-1086 BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent.
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GC31072
Camylofine
Camylofin is an antimuscarinic, is a smooth muscle relaxant
-
GC16937
Carbamoylcholine chloride
Cholinergic receptor agonist
- GC31255 CDD0102 (CDD0102A) CDD0102 (CDD0102A) is a potent M1 Muscarinic receptor agonist.
- GC14215 Cevimeline A muscarinic receptor agonist
- GC43232 Cevimeline (hydrochloride) Cevimeline is a muscarinic receptor agonist (EC50s = 23, 48, and 63 nM for M1, M3, and M5, respectively, and >1 μM for M2 and M4).
- GC17157 Cevimeline hydrochloride hemihydrate
- GC38693 Choline bitartrate Choline bitartrate is a vitamin-like essential nutrient, can affect diseases such as liver disease, atherosclerosis and neurological disorders.
- GC30955 Cimetropium Bromide (DA-3177) Cimetropium Bromide (DA-3177) (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
- GC31048 Clidinium bromide (Ro 2-3773) Clidinium bromide (Ro 2-3773) is a quaternary amine antimuscarinic agent.
- GC17760 Clozapine Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia.
- GC50193 Clozapine - d8 Clozapine - d8 (HF 1854-d8) is the deuterium labeled Clozapine.
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GC10822
Clozapine N-oxide (CNO)
A metabolite of clozapine and muscarinic DREADD agonist
- GC31209 Cyclodrine hydrochloride Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.
- GC43347 Cyclopentolate (hydrochloride) Cyclopentolate is an antagonist of muscarinic acetylcholine receptors (Kis = 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively).
- GC31136 Darenzepine Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.
- GC35810 Darifenacin Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
- GC15772 Darifenacin HBr Darifenacin HBr (UK-88525 hydrobromide) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
- GC60758 Deschloroclozapine Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist.
- GC35842 Desfesoterodine Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively.
- GC35845 Dexetimide Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinity muscarinic receptor antagonist.
- GC16635 Diphemanil Methylsulfate Diphemanil methylsulfate is a quaternary ammonium anticholinergic.
- GC10300 Diphenidol HCl Diphenidol HCl (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity.
- GC30849 DREADD agonist 21 A muscarinic hM3Dq DREADD agonist
- GC50446 DREADD agonist 21 dihydrochloride Potent muscarinic DREADD agonist; water soluble version of DREADD agonist 21
- GC16073 Dronedarone An antiarrhythmic agent
- GC30409 Elucaine Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
-
GC63484
Emraclidine
Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11).
- GC31017 ENS-163 phosphate (ENS 213-163) ENS-163 phosphate (ENS 213-163) is a selective muscarinic M1 receptor agonist.
- GC39379 Fesoterodine Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively.
- GC16087 Fesoterodine Fumarate Muscarinic AChR receptor antagonist
- GC39380 Fesoterodine L-mandelate Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively.
- GC13361 Flavoxate hydrochloride muscarinic AChR antagonist
- GC11385 G-Protein antagonist peptide Inhibits G protein activation by GPCRs
- GC63766 G-Protein antagonist peptide TFA G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding.
- GC10972 Gallamine Triethiodide Cholinergic receptor blocker
- GC15029 Glycopyrrolate Muscarinic competitive antagonist
- GC65379 Guvacoline hydrochloride Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors.
- GC13897 Homatropine Bromide Muscarinic AChR antagonist
- GC17908 Homatropine Methylbromide Muscarinic AChR antagonist
- GC11035 Hyoscyamine Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist.
- GC30812 Imidafenacin (KRP-197) Imidafenacin (KRP-197)(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).
- GC12717 Ipratropium Bromide AChR antagonist
- GC68326 Ipratropium-d3 bromide
- GC13191 Irsogladine PDE4 inhibitor
- GC33878 Irsogladine maleate (Dicloguamine maleate) Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.
- GC39076 Isopteropodine Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.
- GC50681 JHU 37152 JHU 37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5nM and 0.5nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively.
- GC50682 JHU 37160 JHU 37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5nM and 0.2nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively.
- GC39130 L-Hyoscyamine sulfate L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist.
- GC65504 L-Hyoscyamine-d3
- GC36442 Levetimide Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM.
- GC17779 Levetiracetam Antiepileptic drug
- GC13445 LY2119620 positive allosteric modulator of M2/M4 receptor
- GC31984 M3 receptor antagonist 1 M3 receptor antagonist 1 is a selective, long-acting and competitive muscarinic M3 receptor antagonist.
- GC65567 M4 mAChR agonist-1 M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC50 >10 μM for human M4.
- GC36523 mAChR-IN-1 mAChR-IN-1 is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM.
- GC36524 mAChR-IN-1 hydrochloride mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM.
- GC67620 Methacholine bromide Methacholine (Acetyl-β-methylcholine) bromide is a potent muscarinic-3 (M3) agonist. Methacholine bromide acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine bromide shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine bromide 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.
- GC33434 Methacholine chloride Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist.
- GC17825 Methscopolamine Muscarinic acetylcholine receptor blocker
- GC31946 Methylbenactyzium Bromide Methylbenactyzium Bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor.
- GC30968 Metixene hydrochloride hydrate Metixene (Piperidine) hydrochloride hydrate is an anticholinergic and antiparkinsonian agent.
- GC30446 MHP 133 MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
- GC67979 MK-6884
- GC30836 MK-7622 (M1 receptor modulator) MK-7622 (M1 receptor modulator) (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
- GC61802 ML380 ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively.
- GC68335 N-Demethyl MK-6884
- GC16553 N-Desmethylclozapine 5-HT2C serotonin receptor antagonist
- GC38933 Nebracetam hydrochloride Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca2+ concentration.
- GC32667 Nuvenzepine Nuvenzepine is an mAChR antagonist, has the potential for gastrospasm treatment.
- GC61809 Olanzapine D3 Olanzapine D3 (LY170053-d3) is the deuterium labeled Olanzapine.
- GC10863 Otilonium Bromide AChR inhibitor
-
GC32049
Oxitropium Bromide
Oxitropium bromide is an mAChR antagonist used as an anticholinergic bronchodilator drug for the treatment of asthma and chronic obstructive pulmonary disease.
- GC38658 Oxotremorine M iodide A muscarinic receptor agonist and KCNQ2/3 potassium channel blocker