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AChR

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AChR Products

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AChR Inhibitors (66)
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AChR Antagonists (47)
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AChR Modulators (12)
New AChR Products

Catalog No.	Product Name	Information	Product Use Citations
S4505	Vinblastine sulfate	Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.	Int J Mol Sci, 2025, 26(8)3864 Anticancer Res, 2025, 45(1):39-53 iScience, 2024, 27(10):110862
S1351	Ivermectin	Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.	Viruses, 2025, 17(2)220 J Clin Invest, 2024, 134(22)e181314 Viruses, 2024, 16(4)640
S2462	Donepezil HCl	Donepezil HCl is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.	Sci Adv, 2025, 11(14):eads7191 Theranostics, 2023, 13(6):1826-1842 J Cell Physiol, 2023, 10.1002/jcp.31057
S2629	PNU-120596	PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.	Front Med (Lausanne), 2021, 8:642960 J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916
S4231	Pilocarpine HCl	Pilocarpine HCl (NSC 5746) is a selective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.	Viruses, 2024, 16(10)1559 Heliyon, 2024, 10(1):e23945 Theranostics, 2021, 11(12):5986-6005
S2497	Pancuronium dibromide	Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant.	J Immunother Cancer, 2024, 12(11)e009805 bioRxiv, 2024, 2024.05.23.595327 Biomedicines, 2022, 10(12)3056
S2508	Scopolamine (LSM-4015) HBr	Scopolamine HBr (LSM-4015,NSC 61806,(-)-Scopolamine hydrobromide, Hyoscine hydrobromide, Scopine hydrobromide) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.	Heliyon, 2024, 10(1):e23945 Zool Res, 2023, 44(4):712-724 Zool Res, 2023, 44(4):712-724
S4162	Benzethonium Chloride	Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.	Nat Commun, 2023, 10.1038/s41467-023-42332-0 Nat Commun, 2023, 14(1):6690 iScience, 2023, 26(8):107477
S1356	Levetiracetam (UCB-L059)	Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.	Front Neurosci, 2023, 17:1336026 bioRxiv, 2023, 2023.11.10.566574 Alzheimers Dement (N Y), 2022, 8(1):e12329
S6887	CNO (Clozapine N-oxide)	CNO (Clozapine N-oxide) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist.Solutions are unstable and should be fresh-prepared.	Theranostics, 2025, 15(5):1822-1841 STAR Protoc, 2025, 6(1):103542 Theranostics, 2024, 14(7):2881-2896
S2452	Amfebutamone (Bupropion) HCl	Amfebutamone (Bupropion) HCl(Wellbutrin) is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.	Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433 Front Microbiol, 2020, 10:2936 G3 (Bethesda), 2014, 4(6):1081-9
S5073	Donepezil	Donepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type.	Cell Biosci, 2024, 14(1):146 Theranostics, 2023, 13(6):1826-1842 Front Bioeng Biotechnol, 2022, 10:855755
S1805	Acetylcholine Chloride	The chemical compound Acetylcholine Chloride(ACh chloride) is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans.	Cell Mol Life Sci, 2024, 81(1):88 iScience, 2023, 26(3):106241 Cell, 2022, 185-21:3950-3965.e25
S1978	Methscopolamine	Methscopolamine is a muscarinic acetylcholine receptor blocker.	Mol Brain, 2021, 14(1):113 Mol Neurobiol, 2020, 10.1007/s12035-020-02175-y Neuropharmacology, 2019, 146:252-263
S2455	Bethanechol chloride	Bethanechol chloride(Myocholine,Urecholine) is a selective muscarinic receptor agonist without any effect on nicotinic receptors.	Environ Toxicol Chem, 2021, 10.1002/etc.5018 Exp Physiol, 2020, 10.1113/EP088900 Lung, 2018, 196(2):219-229
S2614	Arecoline HBr	Arecoline(NSC-31750) is a muscarinic acetylcholine receptor agonist.	Antioxidants (Basel), 2024, 13(4)430 Int J Oral Sci, 2024, 16(1):17 Oncogene, 2020, 39(11):2437-2449
S1683	Ipratropium Bromide	Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD).	Int Forum Allergy Rhinol, 2020, 10(2):233-242 Anal Chem, 2019, 91(18):11888-11896
S2130	Atropine sulfate monohydrate	Atropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery.	Neurosci Bull, 2023, none Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S3047	Otilonium Bromide	Otilonium bromide is an antimuscarinic.	Biochem Pharmacol, 2023, 215:115746 Res Microbiol, 2022, S0923-2508(22)00073-0
S2087	Rivastigmine Tartrate	Rivastigmine Tartrate (ENA 713) is a cholinesterase inhibitor with IC50 of 5.5 μM, and used as a parasympathomimetic or cholinergic agent for the treatment of mild to moderate Alzheimer disease.	J Cell Physiol, 2023, 10.1002/jcp.31057 Mol Psychiatry, 2018, 23(3):767-776
S3144	Darifenacin HBr	Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pK_i of 8.9.	AAPS PharmSciTech, 2024, 25(7):204 World J Gastroenterol, 2023, 29(20):3103-3118 JCI Insight, 2017, 2(3):e89780
S4023	Procaine HCl	Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with K_D of 1.7 μM.	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94
S4171	Choline Chloride	Choline chloride(Hepacholine) is a quaternary ammonium salt used as an additive for animal feed. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.	Nat Commun, 2023, 14(1):5034 Nat Commun, 2023, 14(1):5034
S3903	Lycorine	Lycorine (Galanthidine, Amarylline, Narcissine, Licorine, Belamarine) is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis.	Transl Cancer Res, 2024, 13(12):6675-6687 Kaohsiung J Med Sci, 2023, none Acta Pharmacol Sin, 2021, 1-11
S4718	Acetylcholine iodide	Acetylcholine iodide (Acetylcolina) is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.	Food Sci Nutr, 2022, 10(8):2773-2785 Biotechnol Lett, 2020, 42(7):1219-1227
S2251	(-)-Huperzine A (HupA)	(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with K_i of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.	Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
S1440	Varenicline Tartrate (CP 526555-18)	Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction.	Neuropharmacology, 2023, S0028-3908(23)00262-9
S1339	Galanthamine HBr	Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.	J Cell Physiol, 2023, 10.1002/jcp.31057
S2549	Trospium chloride	Trospium chloride is a competitive muscarinic cholinergic receptor antagonist.	J Immunother Cancer, 2024, 12(11)e009805 FEBS Lett, 2020, 10.1002/1873-3468.14015
S2471	Gallamine Triethiodide	Gallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM.	Mol Cell, 2019, 75(1):53-65
S2490	Neostigmine Bromide	Neostigmine Bromide is a reversible acetylcholinesterase inhibitor.	Am J Physiol Gastrointest Liver Physiol, 2016, 310(3):G181-92
S4014	Hyoscyamine	Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM.	Theranostics, 2022, 12(12):5488-5503
S4713	Atropine	Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.	Front Mol Biosci, 2024, 11:1423351 iScience, 2023, 26(3):106241
S4024	Homatropine Methylbromide	Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.	Nature, 2018, 560(7718):372-376
S4121	Succinylcholine Chloride Dihydrate	Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.	Cell Rep Methods, 2023, 3(10):100599
S5900	Edrophonium chloride	Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase.	Front Mol Biosci, 2024, 11:1423351 Int J Mol Sci, 2023, 10.3390/ijms242115535
S4422	Nitenpyram	Nitenpyram(Bestguard,Capstar) is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.	Proc Natl Acad Sci U S A, 2020, 117(21):11321-11327
S2287	Cytisine	Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist.	Transl Oncol, 2023, 35:101712
S4660	Glycopyrrolate	Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.	J Clin Med, 2022, 11(9)2307
S6432	Cevimeline HCl hemihydrate	Cevimeline HCl hemihydrate(AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.	Front Pharmacol, 2022, 13:914153
S4687	Rivastigmine	Rivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).	Front Mol Biosci, 2024, 11:1423351 Nature, 2018, 560(7718):372-376
S3117	Oxybutynin hydrochloride	Oxybutynin(MJ4309-1) is an anticholinergic medication used to relieve urinary and bladder difficulties.	Environ Toxicol Chem, 2021, 10.1002/etc.5018
S9154	Chelidonine	Chelidonine (Stylophorin, Helidonine), a major bioactive, isoquinoline alkaloid ingredient in Chelidonium majus, exhibits anti-inflammatory properties and acetylcholinesterase and butyrylcholinesterase inhibitory activity.	Onco Targets Ther, 2019, 12:6685-6697
S3866	Galanthamine	Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.
S5493	Atropine sulfate	Atropine Sulfate (Sulfatropinol, Atropette, Tropintran) is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects.	Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S2547	Tiotropium Bromide hydrate	Tiotropium Bromide hydrate (BA 679BR) is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.
S1754	Oxybutynin	Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties.
S3048	Solifenacin succinate	Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class.	J Immunother Cancer, 2024, 12(11)e009805
S1405	Vecuronium Bromide	Vecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.
S2378	Butylscopolamine Bromide	Butylscopolamine Bromide (Scopolamine Butylbromide,(-)-Scopolamine butylbromide, Hyoscine butylbromide), is a peripherally acting antimuscarinic, anticholinergic agent used as an abdominal-specific antispasmodic.
S4031	Aclidinium Bromide	Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with K_i of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.
S1397	Rocuronium Bromide	Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia.	Cureus, 2024, 16(12):e76537
S1929	Irsogladine	Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
F2910^New	Muscarinic Acetylcholine Receptor 2/CM2 Rabbit mAb	Muscarinic Acetylcholine Receptor 2/CM2,Muscarinic Acetylcholine Receptor m2
E0524	Spinosad	Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete, is a biological neurotoxic insecticide with a broader action spectrum, targeting the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system.
S5873	Scopolamine HBr trihydrate	Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
S3202	Catharanthine	Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.	iScience, 2024, 27(10):110862
S0717	Varenicline (CP 526555) dihydrochloride	Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.
S4575	Pralidoxime chloride	Pralidoxime chloride (2-PAM) is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator.
S0720	PNU-282987	PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM.
S3245	Nodakenetin	Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S4931	Propiverine hydrochloride	Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence. Propiverine is a muscarinic receptor antagonist possessing additional properties, i.e., block of L-type Ca2+ channels.
S0518	NS 1738	NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nicotinic acetylcholine receptor (α7 nAChR), with respect to positive modulation of Xenopus laevis oocyte α7 nAChR with EC50 of 3.4 μM, as well as a comparable efficacy at the rat α7 nAChR with EC50 of 3.9 μM.
E3551	Stephania Extract	Stephania Extract is extracted from Stephania, which ameliorates Scopolamine-Induced Memory Impairment in Mice through Inhibition of Acetylcholinesterase and Oxidative Stress.
S9219	Huperzine B	Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.
S0521	PNU-282987 S enantiomer free base	PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base, which is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
S5886	Hodostin	Hodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis.
S0032	Batefenterol	Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively.
S3246	Picfeltarraenin IB	Picfeltarraenin IB, a cucurbitacin glycoside isolated from Picriafel-terrae, is an inhibitor of acetylcholinesterase (AChE). Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation.
S5480	Clidinium Bromide	Clidinium Bromide(Ro 2-3773) is an anticholinergic drug.
S5385	Imidafenacin	Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(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). IC50 value: 0.3 nM(M3).
S6985	Varenicline	Varenicline(CP 526555) is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors.
S4025	Homatropine Bromide	Homatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
E4822^New	Tacrine	Tacrine is a potent acetylcholinesterase (AChE) inhibitor. It inhibits acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) with an IC50 of 77 nM and 69 nM, respectively. It is used in the treatment of Alzheimer's disease (AD), also poisoning topoisomerases and inhibiting in vivo (mitochondrial)mtDNA synthesis.
S4027	Flavoxate HCl	Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM.	Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433
S9326	Scopolamine	Scopolamine (Skopolamin) is a tropane alkaloid derived from plants of the nightshade family, specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties.	Immunity, 2024, 57(2):364-378.e9
S5238	Solifenacin (YM905)	Solifenacin (YM905) is a competitive muscarinic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle.
S3820	Dehydroevodiamine hydrochloride	Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production.
S5258	Revefenacin	Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.
S2054	Orphenadrine Citrate	Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.
S4034	Diphemanil Methylsulfate	Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).
E3651	Lycopodiastrum casuarinoides Extract	Lycopodiastrum casuarinoides Extract is extracted from Lycopodiastrum casuarinoides, which has acetylcholinesterase inhibitory activity.
E6020^New	(±)-Darifenacin	Darifenacin [(±)-UK-88525] is a potent, specific and competitive M3 selective receptor antagonist (M3 SRA) that has been shown to have high affinity and selectivity for the M3 receptor. It significantly improves major overactive bladder (OAB) symptoms with proven efficacy, tolerability, and safety.
S9252	Corydaline	Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers.
E7262^New	Darifenacin	Darifenacin (UK-88525) is a selective and orally active antagonist of M3 muscarinic receptor (M3R) with a pKi of 8.86. It exhibits efficacy in overactive bladder, partly due to bladder afferent desensitization. It also shows potential in preventing liver injury and inhibiting colorectal cancer growth in both in vitro and in vivo models.	World J Gastroenterol, 2023, 29(20):3103-3118
S1832	Atracurium Besylate	Atracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.
S0552	BNC210	BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR).
S0766	RHC 80267	RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC).
S9260	Nodakenin	Nodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM.
S5022	Varenicline Hydrochloride	Varenicline (CP 526555) Hydrochloride is a partial agonist of α4β2 nicotine acetylcholine receptor (nAChR) and α6β2 nicotine acetylcholine receptor (nAChR), with a Ki value of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively, in the striatum of rats.
S4143	Pentoxyverine Citrate	Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.
S3835	Loganin	Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively.
S6518	Desmethylanethol trithione	Desmethylanethol trithione (ADT-OH) is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor.
F2495^New	Acetylcholinesterase Rabbit mAb
E3116	Acanthopanax Senticosus Extract	Acanthopanax Senticosus Extract is obtained from Acanthopanax Senticosus, which exhibits dual effects of contraction via muscarinic ACh receptors (mAChRs) and direct relaxation on mouse ileal function, and its relaxant effect could be useful in treating diarrhea symptoms, resulting in an increase in the parasympathetic nerve activities.
S4619	Itopride hydrochloride	Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
E1876	GTS-21 dihydrochloride	GTS-21 dihydrochloride(DMXB-A, DMBX-anabaseine) is a selective agonist of alpha7 nicotinic acetylcholine receptor (α7-nAChR) and exhibits anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also an antagonist of α4β2 with a Ki value of 20 nM for humanα4β2 and 5-HT3A receptor with an IC50 value of 3.1 μM.
S0782	VU0238441	VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively.
S0783	VU0119498	VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively.
S5777	Ipratropium bromide monohydrate	Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively.
S7366	LY2119620	LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
S9459	Mecamylamine Hydrochloride	Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR(nicotinic acetylcholine receptors) antagonist.It is also a ganglionic blocker and can across the blood-brain barrier. It can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
E3612	Cremastra appendiculata Extract	Cremastra Appendiculata Extract is extracted from Cremastra appendiculata (Pseudobulbus Cremastrae seu Pleiones), the dried pseudostem of plants of the Orchidaceae family. Cremastra appendiculata has antibacterial, antihypertensive, gout, antitumor, and acetylcholine receptor M3-blocking effects. The extract of cremastra appendiculata can be used to treat Lewis lung cancer, liver cancer, and breast cancer.
E0829	Nitrocaramiphen hydrochloride	Nitrocaramiphen hydrochloride is an antagonist of muscarinic acetylcholine receptor M1 (mAChR M1), which can completely remove the hyperpolarizing effect of muscarine.
E2874	Sofpironium bromide	Sofpironium bromide (BBI 4000) is an anticholinergic agent that reduces sweat by inhibiting M3 muscarinic receptors in eccrine glands.
E0755	Guvacoline hydrochloride	Norarecoline hydrochloride (Guvacoline hydrochloride) is a pyridine alkaloid found in Areca triandra, which can act as a full agonist at both atrial and ileal muscarinic receptors.
E4714^New	Xanomeline	Xanomeline(LY-246708) is a selective agonist of muscarinic type 1(M(1) receptor and muscarinic type 4 receptor(M(4). It increases neuronal excitability and inhibits behaviors induced by D-amphetamine and (-)-apomorphine.
S3701	Benactyzine hydrochloride	Benactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety.
S5699	Scopolamine N-Oxide HydrobroMide Monohydrate	Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
S3913	Pimethixene maleate	Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
E3223	Alpiniae Officinarum Rhizoma Extract	Alpiniae Officinarum Rhizoma Extract is extracted from Alpiniae Officinarum Rhizoma, which inhibits acetylcholinesterase (AChE) and can be used for the treatment of Alzheimer's disease.
S4623	Methylbenactyzine Bromide	Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity.
E0799	VU 0365114	VU 0365114 is a muscarinic acetylcholine receptor M5-preferring (mAChR M5-preferring) positive allosteric modulator (PAM) with an EC50 of 2.7 μM.
E4298	(-)-Carvone	(-)-Carvone is an insect neurotoxin and is an irreversible inhibitor of acetylcholinesterase (AChE). It can be used as a bird repellent, inhibits larval growth, decreases pupation rate, and increases the mortality of larvae.
S3639	Tacrine hydrochloride hydrate	Tacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) is a centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. It also acts as a histamine N-methyltransferase inhibitor.
S4069	Hexamethonium Dibromide	Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.
S4072	Decamethonium Bromide	Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
S3662	Pirenzepine dihydrochloride	Pirenzepine is an antimuscarinic agent which inhibits gastric acid secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular and urinary functions.
S9789	JHU37152	JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
S9790	JHU37160	JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
E1265	Deschloroclozapine	Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs (muscarinic Designer Receptors Exclusively Activated by Designer Drugs) agonist, and binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively.
S3311	Myosmine	Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM.
S3769	Palmatine	Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.	Eur J Pharmacol, 2024, 967:176395
E0382	W-84 Dibromide	W-84 dibromide (HDMPPA) is a potent allosteric modulator of M2-acetylcholine receptors, which retards 3HN-methylscopolamine dissociation.
S9069	Jatrorrhizine chloride	Jatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.
S5850	Vasicine	Vasicine, an alkaloid isolated from A. vasica, is a potential natural cholinesterase inhibitor, exhibits promising anticholinesterase activity in preclinical models and has been in development for treatment of Alzheimer’s disease.
S3788	Carvacrol	Carvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities.
S9087	Tenuifolin	Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production.
S4804	1-Naphthyl acetate	1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages. 1-Naphthyl acetate is a potent chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity.
S3884	Jatrorrhizine	Jatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.
S3684	Methacholine chloride	Methacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors.
E5792^New	BAY 2413555	BAY 2413555 is a first selective positive allosteric modulator of the muscarinic acetylcholine receptor (M2R) to restore cardiac autonomic balance. It also inhibits CYP2C8 and CYP2C9 with IC50 values of 17 µM and 13 µM, respectively.
S4703	Choline bitartrate	Choline bitartrate (2-hydroxyethyl(trimethyl)azanium, 2,3,4-trihydroxy-4-oxobutanoate) is a form of the nutrient choline which is found in foods. Choline is necessary for normal liver and kidney function and a component of the neurotransmitter acetylcholine, a chemical that facilitates communication between the nerves and muscles.
S5930	PNU 282987 HCl	PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
S5931	BQCA	BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S3735	Umeclidinium bromide	Umeclidinium bromide(GSK573719A) is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
S5538	Tropisetron	Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.	Chin Med, 2024, 19(1):87 Neural Regen Res, 2023, 18(9):2019-2028
S5075	Acotiamide	Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
S4357	Tacrine HCl	Tacrine is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
S2957	Encenicline (EVP-6124) hydrochloride	Encenicline (EVP-6124) hydrochloride is a selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors.
E0176	Dinotefuran	Dinotefuran (MTI-446), a neonicotinoid, is an effective nAChRs agonist with EC50 of 7.8 μM and shows high insecticidal activity on Da2b2 hybrid nAChRs.
E0831	Pseudocoptisine chloride	Pseudocoptisine chloride (Isocoptisine chloride) is a quaternary alkaloid with benzylisoquinoline skeleton isolated from Corydalis Tuber, inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM, showing anti-inflammatory and anti-amnestic effects.
E2237	Vasicine (hydrochloride)	Vasicine hydrochloride(Peganine hydrochloride) is a salt of vasicine (VAS), an alkaloid isolated from Adhatoda vasica, is a potential natural cholinesterase inhibitor. VAS inhibits both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
S3904	Isoimperatorin	Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM.
S4834	Propantheline bromide	Propantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan) is a muscarinic antagonist used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia.
S9138	Picfeltarraenin IA	Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system.
S4542	Trihexyphenidyl hydrochloride	Trihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class.	Cell Commun Signal, 2024, 22(1):551
S5511	Ethyl (triphenylphosphoranylidene) acetate	Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE.
S4992	Nanofin	Nanofin (2,6-Dimethylpiperidine, Lupetidine, Naniopinum) is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension.
S6469	Thonzylamine	Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
S0457	DREADD agonist 21	DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.
S2082	Adiphenine HCl	Adiphenine HCl(NSC 129224) is a nicotinic receptor inhibitor, used as an antispasmodic drug.
S9475	Hupehenine	Hupehenine is a steriodal alkaloid extracted from the bulbs of Fritillaria Hupehensis, with the potential for inhibiting acetylcholine, antagonism for muscarinic receptors and cholinesterase inhibition.
S0016	SN-6	SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S5100	Pralidoxime Iodide	Pralidoxime Iodide (2-PAM) is an antidote approved for reactivation of inhibited acetylcholinesterase (AChE) in organophosphate poisoning.
S4389	Bephenium Hydroxynaphthoate	Bephenium(NSC 759245) is an activator of B-type Acetylcholine receptor (AChR). Bephenium selectively activates the Hco-L-AChR1 subtype made of Hco-UNC-29.1, Hco-UNC-38, Hco-UNC-63, Hco-ACR-8 subunits. Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis.
S5747	Morantel tartrate	Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S3298	Caulophylline (N-Methylcytisine)	Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.
S9560	Anisodamine Hydrobromide	Anisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
S5921	Cyclopentolate Hydrochloride	Cyclopentolate is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively.
E7001^New	Pilocarpine	Pilocarpine is a non-selective agonist of muscarinic acetylcholine receptor (mAChR), commonly used to treat xerostomia and glaucoma. It modulates the electrical properties of heart cells, likely by activating a potassium (K+) current mediated by M3 receptors.	Front Mol Biosci, 2024, 11:1423351
E4774^New	4-DAMP	4-DAMP (4-diphenyl-acetoxy-N-methyl-piperidine) (4-DAMP methiodide) is a selective antagonist of M3 type muscarinic acetylcholine receptors (M3-mAChR) with a pKi of 9.3. It also has a high affinity for the closely-related M5 receptor with a pKi of 8.9. It is routinely used to study the regulation and functions of the M3 receptor.
S4838	Acotiamide hydrochloride	Acotiamide Hydrochloride (YM-443, Z-338) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor.
S9179	Catharanthine hemitartrate	Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine.
S4292	Diphenidol HCl	Diphenidol HCl(Diphenidol hydrochloride) is a potent antagonist of muscarinic M2 and M3 receptor with pK_b of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.
S6795	VU0357017 Hydrochloride	VU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM.
E5819^New	Clozapine N-oxide dihydrochloride	Clozapine N-oxide dihydrochloride is a primary metabolite of clozapine. It acts as an agonist for human muscarinic designer receptors DREADD, with a pEC50 of 8.31 for the M1 DREADD.
S2646	VU0238429	VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4.
S1913	Tropicamide	Tropicamide(Ro 1-7683) is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.
S4505	Vinblastine sulfate	Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.	Int J Mol Sci, 2025, 26(8)3864 Anticancer Res, 2025, 45(1):39-53 iScience, 2024, 27(10):110862
S2462	Donepezil HCl	Donepezil HCl is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.	Sci Adv, 2025, 11(14):eads7191 Theranostics, 2023, 13(6):1826-1842 J Cell Physiol, 2023, 10.1002/jcp.31057
S4162	Benzethonium Chloride	Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.	Nat Commun, 2023, 10.1038/s41467-023-42332-0 Nat Commun, 2023, 14(1):6690 iScience, 2023, 26(8):107477
S2452	Amfebutamone (Bupropion) HCl	Amfebutamone (Bupropion) HCl(Wellbutrin) is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.	Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433 Front Microbiol, 2020, 10:2936 G3 (Bethesda), 2014, 4(6):1081-9
S5073	Donepezil	Donepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type.	Cell Biosci, 2024, 14(1):146 Theranostics, 2023, 13(6):1826-1842 Front Bioeng Biotechnol, 2022, 10:855755
S3047	Otilonium Bromide	Otilonium bromide is an antimuscarinic.	Biochem Pharmacol, 2023, 215:115746 Res Microbiol, 2022, S0923-2508(22)00073-0
S2087	Rivastigmine Tartrate	Rivastigmine Tartrate (ENA 713) is a cholinesterase inhibitor with IC50 of 5.5 μM, and used as a parasympathomimetic or cholinergic agent for the treatment of mild to moderate Alzheimer disease.	J Cell Physiol, 2023, 10.1002/jcp.31057 Mol Psychiatry, 2018, 23(3):767-776
S4023	Procaine HCl	Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with K_D of 1.7 μM.	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94
S3903	Lycorine	Lycorine (Galanthidine, Amarylline, Narcissine, Licorine, Belamarine) is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis.	Transl Cancer Res, 2024, 13(12):6675-6687 Kaohsiung J Med Sci, 2023, none Acta Pharmacol Sin, 2021, 1-11
S2251	(-)-Huperzine A (HupA)	(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with K_i of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.	Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
S1339	Galanthamine HBr	Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.	J Cell Physiol, 2023, 10.1002/jcp.31057
S2471	Gallamine Triethiodide	Gallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM.	Mol Cell, 2019, 75(1):53-65
S2490	Neostigmine Bromide	Neostigmine Bromide is a reversible acetylcholinesterase inhibitor.	Am J Physiol Gastrointest Liver Physiol, 2016, 310(3):G181-92
S4014	Hyoscyamine	Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM.	Theranostics, 2022, 12(12):5488-5503
S5900	Edrophonium chloride	Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase.	Front Mol Biosci, 2024, 11:1423351 Int J Mol Sci, 2023, 10.3390/ijms242115535
S4687	Rivastigmine	Rivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).	Front Mol Biosci, 2024, 11:1423351 Nature, 2018, 560(7718):372-376
S9154	Chelidonine	Chelidonine (Stylophorin, Helidonine), a major bioactive, isoquinoline alkaloid ingredient in Chelidonium majus, exhibits anti-inflammatory properties and acetylcholinesterase and butyrylcholinesterase inhibitory activity.	Onco Targets Ther, 2019, 12:6685-6697
S3866	Galanthamine	Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.
S5493	Atropine sulfate	Atropine Sulfate (Sulfatropinol, Atropette, Tropintran) is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects.	Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S2378	Butylscopolamine Bromide	Butylscopolamine Bromide (Scopolamine Butylbromide,(-)-Scopolamine butylbromide, Hyoscine butylbromide), is a peripherally acting antimuscarinic, anticholinergic agent used as an abdominal-specific antispasmodic.
S4031	Aclidinium Bromide	Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with K_i of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.
S1397	Rocuronium Bromide	Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia.	Cureus, 2024, 16(12):e76537
S1929	Irsogladine	Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S3202	Catharanthine	Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.	iScience, 2024, 27(10):110862
S3245	Nodakenetin	Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
E3551	Stephania Extract	Stephania Extract is extracted from Stephania, which ameliorates Scopolamine-Induced Memory Impairment in Mice through Inhibition of Acetylcholinesterase and Oxidative Stress.
S9219	Huperzine B	Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.
S5886	Hodostin	Hodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis.
S3246	Picfeltarraenin IB	Picfeltarraenin IB, a cucurbitacin glycoside isolated from Picriafel-terrae, is an inhibitor of acetylcholinesterase (AChE). Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation.
S5385	Imidafenacin	Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(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). IC50 value: 0.3 nM(M3).
E4822^New	Tacrine	Tacrine is a potent acetylcholinesterase (AChE) inhibitor. It inhibits acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) with an IC50 of 77 nM and 69 nM, respectively. It is used in the treatment of Alzheimer's disease (AD), also poisoning topoisomerases and inhibiting in vivo (mitochondrial)mtDNA synthesis.
S3820	Dehydroevodiamine hydrochloride	Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production.
E3651	Lycopodiastrum casuarinoides Extract	Lycopodiastrum casuarinoides Extract is extracted from Lycopodiastrum casuarinoides, which has acetylcholinesterase inhibitory activity.
S9252	Corydaline	Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers.
S1832	Atracurium Besylate	Atracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.
S0766	RHC 80267	RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC).
S9260	Nodakenin	Nodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM.
S3835	Loganin	Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively.
S4619	Itopride hydrochloride	Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
E3612	Cremastra appendiculata Extract	Cremastra Appendiculata Extract is extracted from Cremastra appendiculata (Pseudobulbus Cremastrae seu Pleiones), the dried pseudostem of plants of the Orchidaceae family. Cremastra appendiculata has antibacterial, antihypertensive, gout, antitumor, and acetylcholine receptor M3-blocking effects. The extract of cremastra appendiculata can be used to treat Lewis lung cancer, liver cancer, and breast cancer.
E2874	Sofpironium bromide	Sofpironium bromide (BBI 4000) is an anticholinergic agent that reduces sweat by inhibiting M3 muscarinic receptors in eccrine glands.
S3913	Pimethixene maleate	Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
E3223	Alpiniae Officinarum Rhizoma Extract	Alpiniae Officinarum Rhizoma Extract is extracted from Alpiniae Officinarum Rhizoma, which inhibits acetylcholinesterase (AChE) and can be used for the treatment of Alzheimer's disease.
E4298	(-)-Carvone	(-)-Carvone is an insect neurotoxin and is an irreversible inhibitor of acetylcholinesterase (AChE). It can be used as a bird repellent, inhibits larval growth, decreases pupation rate, and increases the mortality of larvae.
S3639	Tacrine hydrochloride hydrate	Tacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) is a centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. It also acts as a histamine N-methyltransferase inhibitor.
S3662	Pirenzepine dihydrochloride	Pirenzepine is an antimuscarinic agent which inhibits gastric acid secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular and urinary functions.
S3311	Myosmine	Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM.
S3769	Palmatine	Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.	Eur J Pharmacol, 2024, 967:176395
S9069	Jatrorrhizine chloride	Jatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.
S5850	Vasicine	Vasicine, an alkaloid isolated from A. vasica, is a potential natural cholinesterase inhibitor, exhibits promising anticholinesterase activity in preclinical models and has been in development for treatment of Alzheimer’s disease.
S3788	Carvacrol	Carvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities.
S9087	Tenuifolin	Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production.
S3884	Jatrorrhizine	Jatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.
S5075	Acotiamide	Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
S4357	Tacrine HCl	Tacrine is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
E0831	Pseudocoptisine chloride	Pseudocoptisine chloride (Isocoptisine chloride) is a quaternary alkaloid with benzylisoquinoline skeleton isolated from Corydalis Tuber, inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM, showing anti-inflammatory and anti-amnestic effects.
E2237	Vasicine (hydrochloride)	Vasicine hydrochloride(Peganine hydrochloride) is a salt of vasicine (VAS), an alkaloid isolated from Adhatoda vasica, is a potential natural cholinesterase inhibitor. VAS inhibits both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
S3904	Isoimperatorin	Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM.
S9138	Picfeltarraenin IA	Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system.
S4542	Trihexyphenidyl hydrochloride	Trihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class.	Cell Commun Signal, 2024, 22(1):551
S5511	Ethyl (triphenylphosphoranylidene) acetate	Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE.
S2082	Adiphenine HCl	Adiphenine HCl(NSC 129224) is a nicotinic receptor inhibitor, used as an antispasmodic drug.
S0016	SN-6	SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S9560	Anisodamine Hydrobromide	Anisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
S4838	Acotiamide hydrochloride	Acotiamide Hydrochloride (YM-443, Z-338) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor.
S9179	Catharanthine hemitartrate	Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine.
S4575	Pralidoxime chloride	Pralidoxime chloride (2-PAM) is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator.
S5100	Pralidoxime Iodide	Pralidoxime Iodide (2-PAM) is an antidote approved for reactivation of inhibited acetylcholinesterase (AChE) in organophosphate poisoning.
S4389	Bephenium Hydroxynaphthoate	Bephenium(NSC 759245) is an activator of B-type Acetylcholine receptor (AChR). Bephenium selectively activates the Hco-L-AChR1 subtype made of Hco-UNC-29.1, Hco-UNC-38, Hco-UNC-63, Hco-ACR-8 subunits. Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis.
S2497	Pancuronium dibromide	Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant.	J Immunother Cancer, 2024, 12(11)e009805 bioRxiv, 2024, 2024.05.23.595327 Biomedicines, 2022, 10(12)3056
S2508	Scopolamine (LSM-4015) HBr	Scopolamine HBr (LSM-4015,NSC 61806,(-)-Scopolamine hydrobromide, Hyoscine hydrobromide, Scopine hydrobromide) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.	Heliyon, 2024, 10(1):e23945 Zool Res, 2023, 44(4):712-724 Zool Res, 2023, 44(4):712-724
S1978	Methscopolamine	Methscopolamine is a muscarinic acetylcholine receptor blocker.	Mol Brain, 2021, 14(1):113 Mol Neurobiol, 2020, 10.1007/s12035-020-02175-y Neuropharmacology, 2019, 146:252-263
S1683	Ipratropium Bromide	Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD).	Int Forum Allergy Rhinol, 2020, 10(2):233-242 Anal Chem, 2019, 91(18):11888-11896
S2130	Atropine sulfate monohydrate	Atropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery.	Neurosci Bull, 2023, none Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S3144	Darifenacin HBr	Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pK_i of 8.9.	AAPS PharmSciTech, 2024, 25(7):204 World J Gastroenterol, 2023, 29(20):3103-3118 JCI Insight, 2017, 2(3):e89780
S2549	Trospium chloride	Trospium chloride is a competitive muscarinic cholinergic receptor antagonist.	J Immunother Cancer, 2024, 12(11)e009805 FEBS Lett, 2020, 10.1002/1873-3468.14015
S4713	Atropine	Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.	Front Mol Biosci, 2024, 11:1423351 iScience, 2023, 26(3):106241
S4024	Homatropine Methylbromide	Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.	Nature, 2018, 560(7718):372-376
S4660	Glycopyrrolate	Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.	J Clin Med, 2022, 11(9)2307
S3117	Oxybutynin hydrochloride	Oxybutynin(MJ4309-1) is an anticholinergic medication used to relieve urinary and bladder difficulties.	Environ Toxicol Chem, 2021, 10.1002/etc.5018
S2547	Tiotropium Bromide hydrate	Tiotropium Bromide hydrate (BA 679BR) is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.
S1754	Oxybutynin	Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties.
S3048	Solifenacin succinate	Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class.	J Immunother Cancer, 2024, 12(11)e009805
S5873	Scopolamine HBr trihydrate	Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
S4931	Propiverine hydrochloride	Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence. Propiverine is a muscarinic receptor antagonist possessing additional properties, i.e., block of L-type Ca2+ channels.
S0032	Batefenterol	Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively.
S5480	Clidinium Bromide	Clidinium Bromide(Ro 2-3773) is an anticholinergic drug.
S6985	Varenicline	Varenicline(CP 526555) is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors.
S4025	Homatropine Bromide	Homatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
S4027	Flavoxate HCl	Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM.	Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433
S9326	Scopolamine	Scopolamine (Skopolamin) is a tropane alkaloid derived from plants of the nightshade family, specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties.	Immunity, 2024, 57(2):364-378.e9
S5238	Solifenacin (YM905)	Solifenacin (YM905) is a competitive muscarinic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle.
S5258	Revefenacin	Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.
S2054	Orphenadrine Citrate	Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.
S4034	Diphemanil Methylsulfate	Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).
E6020^New	(±)-Darifenacin	Darifenacin [(±)-UK-88525] is a potent, specific and competitive M3 selective receptor antagonist (M3 SRA) that has been shown to have high affinity and selectivity for the M3 receptor. It significantly improves major overactive bladder (OAB) symptoms with proven efficacy, tolerability, and safety.
E7262^New	Darifenacin	Darifenacin (UK-88525) is a selective and orally active antagonist of M3 muscarinic receptor (M3R) with a pKi of 8.86. It exhibits efficacy in overactive bladder, partly due to bladder afferent desensitization. It also shows potential in preventing liver injury and inhibiting colorectal cancer growth in both in vitro and in vivo models.	World J Gastroenterol, 2023, 29(20):3103-3118
S4143	Pentoxyverine Citrate	Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.
E3116	Acanthopanax Senticosus Extract	Acanthopanax Senticosus Extract is obtained from Acanthopanax Senticosus, which exhibits dual effects of contraction via muscarinic ACh receptors (mAChRs) and direct relaxation on mouse ileal function, and its relaxant effect could be useful in treating diarrhea symptoms, resulting in an increase in the parasympathetic nerve activities.
S5777	Ipratropium bromide monohydrate	Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively.
S9459	Mecamylamine Hydrochloride	Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR(nicotinic acetylcholine receptors) antagonist.It is also a ganglionic blocker and can across the blood-brain barrier. It can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
E0829	Nitrocaramiphen hydrochloride	Nitrocaramiphen hydrochloride is an antagonist of muscarinic acetylcholine receptor M1 (mAChR M1), which can completely remove the hyperpolarizing effect of muscarine.
S3701	Benactyzine hydrochloride	Benactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety.
S5699	Scopolamine N-Oxide HydrobroMide Monohydrate	Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
S4623	Methylbenactyzine Bromide	Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity.
S4069	Hexamethonium Dibromide	Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.
S3735	Umeclidinium bromide	Umeclidinium bromide(GSK573719A) is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
S5538	Tropisetron	Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.	Chin Med, 2024, 19(1):87 Neural Regen Res, 2023, 18(9):2019-2028
S4834	Propantheline bromide	Propantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan) is a muscarinic antagonist used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia.
S4992	Nanofin	Nanofin (2,6-Dimethylpiperidine, Lupetidine, Naniopinum) is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension.
S6469	Thonzylamine	Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
S3298	Caulophylline (N-Methylcytisine)	Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.
S5921	Cyclopentolate Hydrochloride	Cyclopentolate is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively.
E4774^New	4-DAMP	4-DAMP (4-diphenyl-acetoxy-N-methyl-piperidine) (4-DAMP methiodide) is a selective antagonist of M3 type muscarinic acetylcholine receptors (M3-mAChR) with a pKi of 9.3. It also has a high affinity for the closely-related M5 receptor with a pKi of 8.9. It is routinely used to study the regulation and functions of the M3 receptor.
S4292	Diphenidol HCl	Diphenidol HCl(Diphenidol hydrochloride) is a potent antagonist of muscarinic M2 and M3 receptor with pK_b of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.
S1913	Tropicamide	Tropicamide(Ro 1-7683) is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.
S4231	Pilocarpine HCl	Pilocarpine HCl (NSC 5746) is a selective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.	Viruses, 2024, 16(10)1559 Heliyon, 2024, 10(1):e23945 Theranostics, 2021, 11(12):5986-6005
S1356	Levetiracetam (UCB-L059)	Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.	Front Neurosci, 2023, 17:1336026 bioRxiv, 2023, 2023.11.10.566574 Alzheimers Dement (N Y), 2022, 8(1):e12329
S6887	CNO (Clozapine N-oxide)	CNO (Clozapine N-oxide) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist.Solutions are unstable and should be fresh-prepared.	Theranostics, 2025, 15(5):1822-1841 STAR Protoc, 2025, 6(1):103542 Theranostics, 2024, 14(7):2881-2896
S1805	Acetylcholine Chloride	The chemical compound Acetylcholine Chloride(ACh chloride) is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans.	Cell Mol Life Sci, 2024, 81(1):88 iScience, 2023, 26(3):106241 Cell, 2022, 185-21:3950-3965.e25
S2455	Bethanechol chloride	Bethanechol chloride(Myocholine,Urecholine) is a selective muscarinic receptor agonist without any effect on nicotinic receptors.	Environ Toxicol Chem, 2021, 10.1002/etc.5018 Exp Physiol, 2020, 10.1113/EP088900 Lung, 2018, 196(2):219-229
S2614	Arecoline HBr	Arecoline(NSC-31750) is a muscarinic acetylcholine receptor agonist.	Antioxidants (Basel), 2024, 13(4)430 Int J Oral Sci, 2024, 16(1):17 Oncogene, 2020, 39(11):2437-2449
S4171	Choline Chloride	Choline chloride(Hepacholine) is a quaternary ammonium salt used as an additive for animal feed. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.	Nat Commun, 2023, 14(1):5034 Nat Commun, 2023, 14(1):5034
S4718	Acetylcholine iodide	Acetylcholine iodide (Acetylcolina) is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.	Food Sci Nutr, 2022, 10(8):2773-2785 Biotechnol Lett, 2020, 42(7):1219-1227
S1440	Varenicline Tartrate (CP 526555-18)	Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction.	Neuropharmacology, 2023, S0028-3908(23)00262-9
S4121	Succinylcholine Chloride Dihydrate	Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.	Cell Rep Methods, 2023, 3(10):100599
S4422	Nitenpyram	Nitenpyram(Bestguard,Capstar) is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.	Proc Natl Acad Sci U S A, 2020, 117(21):11321-11327
S2287	Cytisine	Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist.	Transl Oncol, 2023, 35:101712
S6432	Cevimeline HCl hemihydrate	Cevimeline HCl hemihydrate(AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.	Front Pharmacol, 2022, 13:914153
S0717	Varenicline (CP 526555) dihydrochloride	Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.
S0720	PNU-282987	PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM.
S0521	PNU-282987 S enantiomer free base	PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base, which is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
S5022	Varenicline Hydrochloride	Varenicline (CP 526555) Hydrochloride is a partial agonist of α4β2 nicotine acetylcholine receptor (nAChR) and α6β2 nicotine acetylcholine receptor (nAChR), with a Ki value of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively, in the striatum of rats.
E1876	GTS-21 dihydrochloride	GTS-21 dihydrochloride(DMXB-A, DMBX-anabaseine) is a selective agonist of alpha7 nicotinic acetylcholine receptor (α7-nAChR) and exhibits anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also an antagonist of α4β2 with a Ki value of 20 nM for humanα4β2 and 5-HT3A receptor with an IC50 value of 3.1 μM.
S7366	LY2119620	LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
E0755	Guvacoline hydrochloride	Norarecoline hydrochloride (Guvacoline hydrochloride) is a pyridine alkaloid found in Areca triandra, which can act as a full agonist at both atrial and ileal muscarinic receptors.
E4714^New	Xanomeline	Xanomeline(LY-246708) is a selective agonist of muscarinic type 1(M(1) receptor and muscarinic type 4 receptor(M(4). It increases neuronal excitability and inhibits behaviors induced by D-amphetamine and (-)-apomorphine.
S4072	Decamethonium Bromide	Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
S9789	JHU37152	JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
S9790	JHU37160	JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
E1265	Deschloroclozapine	Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs (muscarinic Designer Receptors Exclusively Activated by Designer Drugs) agonist, and binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively.
S3684	Methacholine chloride	Methacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors.
S5930	PNU 282987 HCl	PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
S2957	Encenicline (EVP-6124) hydrochloride	Encenicline (EVP-6124) hydrochloride is a selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors.
E0176	Dinotefuran	Dinotefuran (MTI-446), a neonicotinoid, is an effective nAChRs agonist with EC50 of 7.8 μM and shows high insecticidal activity on Da2b2 hybrid nAChRs.
S0457	DREADD agonist 21	DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.
E7001^New	Pilocarpine	Pilocarpine is a non-selective agonist of muscarinic acetylcholine receptor (mAChR), commonly used to treat xerostomia and glaucoma. It modulates the electrical properties of heart cells, likely by activating a potassium (K+) current mediated by M3 receptors.	Front Mol Biosci, 2024, 11:1423351
S6795	VU0357017 Hydrochloride	VU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM.
E5819^New	Clozapine N-oxide dihydrochloride	Clozapine N-oxide dihydrochloride is a primary metabolite of clozapine. It acts as an agonist for human muscarinic designer receptors DREADD, with a pEC50 of 8.31 for the M1 DREADD.
S1351	Ivermectin	Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.	Viruses, 2025, 17(2)220 J Clin Invest, 2024, 134(22)e181314 Viruses, 2024, 16(4)640
S2629	PNU-120596	PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.	Front Med (Lausanne), 2021, 8:642960 J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916
S0518	NS 1738	NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nicotinic acetylcholine receptor (α7 nAChR), with respect to positive modulation of Xenopus laevis oocyte α7 nAChR with EC50 of 3.4 μM, as well as a comparable efficacy at the rat α7 nAChR with EC50 of 3.9 μM.
S0552	BNC210	BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR).
S0782	VU0238441	VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively.
S0783	VU0119498	VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively.
E0799	VU 0365114	VU 0365114 is a muscarinic acetylcholine receptor M5-preferring (mAChR M5-preferring) positive allosteric modulator (PAM) with an EC50 of 2.7 μM.
E0382	W-84 Dibromide	W-84 dibromide (HDMPPA) is a potent allosteric modulator of M2-acetylcholine receptors, which retards 3HN-methylscopolamine dissociation.
E5792^New	BAY 2413555	BAY 2413555 is a first selective positive allosteric modulator of the muscarinic acetylcholine receptor (M2R) to restore cardiac autonomic balance. It also inhibits CYP2C8 and CYP2C9 with IC50 values of 17 µM and 13 µM, respectively.
S5931	BQCA	BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S5747	Morantel tartrate	Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S2646	VU0238429	VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4.
F2910^New	Muscarinic Acetylcholine Receptor 2/CM2 Rabbit mAb	Muscarinic Acetylcholine Receptor 2/CM2,Muscarinic Acetylcholine Receptor m2
E4822^New	Tacrine	Tacrine is a potent acetylcholinesterase (AChE) inhibitor. It inhibits acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) with an IC50 of 77 nM and 69 nM, respectively. It is used in the treatment of Alzheimer's disease (AD), also poisoning topoisomerases and inhibiting in vivo (mitochondrial)mtDNA synthesis.
E6020^New	(±)-Darifenacin	Darifenacin [(±)-UK-88525] is a potent, specific and competitive M3 selective receptor antagonist (M3 SRA) that has been shown to have high affinity and selectivity for the M3 receptor. It significantly improves major overactive bladder (OAB) symptoms with proven efficacy, tolerability, and safety.
E7262^New	Darifenacin	Darifenacin (UK-88525) is a selective and orally active antagonist of M3 muscarinic receptor (M3R) with a pKi of 8.86. It exhibits efficacy in overactive bladder, partly due to bladder afferent desensitization. It also shows potential in preventing liver injury and inhibiting colorectal cancer growth in both in vitro and in vivo models.	World J Gastroenterol, 2023, 29(20):3103-3118
F2495^New	Acetylcholinesterase Rabbit mAb
E4714^New	Xanomeline	Xanomeline(LY-246708) is a selective agonist of muscarinic type 1(M(1) receptor and muscarinic type 4 receptor(M(4). It increases neuronal excitability and inhibits behaviors induced by D-amphetamine and (-)-apomorphine.
E5792^New	BAY 2413555	BAY 2413555 is a first selective positive allosteric modulator of the muscarinic acetylcholine receptor (M2R) to restore cardiac autonomic balance. It also inhibits CYP2C8 and CYP2C9 with IC50 values of 17 µM and 13 µM, respectively.
E7001^New	Pilocarpine	Pilocarpine is a non-selective agonist of muscarinic acetylcholine receptor (mAChR), commonly used to treat xerostomia and glaucoma. It modulates the electrical properties of heart cells, likely by activating a potassium (K+) current mediated by M3 receptors.	Front Mol Biosci, 2024, 11:1423351
E4774^New	4-DAMP	4-DAMP (4-diphenyl-acetoxy-N-methyl-piperidine) (4-DAMP methiodide) is a selective antagonist of M3 type muscarinic acetylcholine receptors (M3-mAChR) with a pKi of 9.3. It also has a high affinity for the closely-related M5 receptor with a pKi of 8.9. It is routinely used to study the regulation and functions of the M3 receptor.
E5819^New	Clozapine N-oxide dihydrochloride	Clozapine N-oxide dihydrochloride is a primary metabolite of clozapine. It acts as an agonist for human muscarinic designer receptors DREADD, with a pEC50 of 8.31 for the M1 DREADD.

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