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Isoform-selective Inhibitors

AChR Products

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
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).
S1339 Galanthamine HBr Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
S1397 Rocuronium Bromide Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia.
S1608 Pyridostigmine Bromide Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.
J Am Heart Assoc, 2014, 3(3):e000804
S1832 Atracurium Besylate Atracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.
S1929 Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S2082 Adiphenine HCl Adiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug.
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.
Mol Psychiatry, 2018, 23(3):767-776
S2251 (-)-Huperzine A (HupA) (-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki 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
S2452 Amfebutamone (Bupropion) HCl Amfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
Georgia State University, 2014, Chaquettea Felton
S2462 Donepezil HCl Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
Front Bioeng Biotechnol, 2022, 10:855755
Analyst, 2022, 10.1039/d2an00031h
Front Cardiovasc Med, 2021, 8:639541
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
S3047 Otilonium Bromide Otilonium bromide is an antimuscarinic.
S3202 Catharanthine Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.
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.
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.
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.
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.
S3769 Palmatine Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.
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.
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.
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.
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.
Neurotherapeutics, 2021, 10.1007/s13311-021-01052-3
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.
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.
Acta Pharmacol Sin, 2021, 1-11
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.
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.
S4014 Hyoscyamine Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM.
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 KD of 1.7 μM.
Biomol Ther (Seoul), 2016, 24(5):489-94
Biomol Ther (Seoul), 2016, 24(5):489-94
S4031 Aclidinium Bromide Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.
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.
Front Cell Infect Microbiol, 2021, 11:630812
Am J Cancer Res, 2019, 9(11):2397-2412
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.
S4505 Vinblastine (NSC-49842) sulfate Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Cancer Res, 2021, canres.0955.2021
S4542 Trihexyphenidyl hydrochloride Trihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class.
S4619 Itopride hydrochloride Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
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).
Nature, 2018, 560(7718):372-376
S4776 Harmaline Harmaline, a natural occurrence β-carboline alkaloid, is a central nervous system stimulant and an acetylcholinesterase (AChR) inhibitor; also inhibits histamine N-methyltransferase.
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.
S5022 Varenicline Hydrochloride Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively.
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.
Front Bioeng Biotechnol, 2022, 10:855755
Front Cardiovasc Med, 2021, 8:639541
Int J Pharm, 2019, 560:294-305
S5075 Acotiamide Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
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).
S5424 Carbaryl Carbaryl (1-naphthyl methylcarbamate) is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors.
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
S5511 Ethyl (triphenylphosphoranylidene) acetate Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE.
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.
S5900 Edrophonium chloride Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase.
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.
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.
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.
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
S9179 Catharanthine hemitartrate Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine.
S9219 Huperzine B Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.
S9252 Corydaline Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers.
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.
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).
S4389 Bephenium Hydroxynaphthoate Bephenium 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.
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.
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.
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
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.
S1913 Tropicamide Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.
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
S2054 Orphenadrine Citrate Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.
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.
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S2240 Fesoterodine Fumarate Fesoterodine Fumarate (SPM 907) is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.
Hum Mol Genet, 2020, ddaa244
S2497 Pancuronium dibromide Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant.
Elife, 2019, 8e45399
Front Physiol, 2019, 10:1039
Scholars' Bank, 2019, N/A
S2508 Scopolamine (LSM-4015) HBr Scopolamine HBr (LSM-4015, NSC 61806) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
Exp Ther Med, 2020, 20(4):3625-3632
Mol Cell, 2019, 75(1):53-65
Autophagy, 2019, 10.1080/15548627.2019.1630224
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.
S2549 Trospium chloride Trospium chloride is a competitive muscarinic cholinergic receptor antagonist.
FEBS Lett, 2020, 10.1002/1873-3468.14015
S2550 Tolterodine tartrate Tolterodine tartrate (PNU-200583E) is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist.
JCI Insight, 2019, 4(20)
S2659 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) 5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
S3048 Solifenacin succinate Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class.
S3117 Oxybutynin hydrochloride Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S3144 Darifenacin HBr Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
JCI Insight, 2017, 2(3):e89780
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.
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.
S3735 Umeclidinium bromide Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
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
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.
S4034 Diphemanil Methylsulfate Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).
S4069 Hexamethonium Dibromide Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.
S4143 Pentoxyverine Citrate Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.
S4292 Diphenidol HCl Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.
S4623 Methylbenactyzine Bromide Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity.
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.
S4713 Atropine Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.
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.
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.
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.
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.
S5480 Clidinium Bromide Clidinium Bromide is an anticholinergic drug.
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.
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.
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.
S5873 Scopolamine HBr trihydrate Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
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.
S6469 Thonzylamine Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
S6985New Varenicline Varenicline 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.
E0172New Imidacloprid

Imidacloprid is a nicotinic acetylcholine receptor (nAChR) agonist with potent insecticidal activity.
E0176New 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.
S0717 Varenicline (CP 526555) dihydrochloride Varenicline (CP 526555, Chantix, Champix) 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.
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.
Anticancer Res, 2021, 41(2):687-697
PLoS One, 2019, 14(2):e0211644
Sci Rep, 2016, 6:25705
S1440 Varenicline Tartrate (CP 526555-18) Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction.
S1805 Acetylcholine Chloride The chemical compound Acetylcholine Chloride is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans.
Biotechnol Lett, 2020, 42(7):1219-1227
Med Sci Monit, 2019, 25:5389-5400
S2287 Cytisine Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist.
S2455 Bethanechol chloride Bethanechol chloride 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 is a muscarinic acetylcholine receptor agonist.
Oncogene, 2020, 39(11):2437-2449
BMC Mol Cell Biol, 2020, 21(1):80
Oncol Rep, 2015, 33(6):2753-60
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.
S4072 Decamethonium Bromide Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
S4121 Succinylcholine Chloride Dihydrate Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.
S4171 Choline Chloride Choline chloride 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.
S4231 Pilocarpine HCl Pilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.
Theranostics, 2021, 11(12):5986-6005
Mol Brain, 2021, 14(1):113
Anticancer Res, 2021, 41(2):687-697
S4359 Carbamoylcholine chloride (Carbachol) Carbamoylcholine chloride (Carbachol, Carbamylcholine chloride, Carbastat, Miostat) is a cholinergic agonist that mimics the effect of acetylcholine on both the muscarinic and nicotinic receptors.
S4422 Nitenpyram Nitenpyram 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
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.
Biotechnol Lett, 2020, 42(7):1219-1227
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.
S6432 Cevimeline Cevimeline (AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.
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.
S6887 Clozapine N-oxide Clozapine N-oxide (CNO) 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.
S7366 LY2119620 LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
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.
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.
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) 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 has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
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
Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916
J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR
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.
S3972 Lobeline hydrochloride Lobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors.
J Cell Mol Med, 2020, 10.1111/jcmm.16029
S5747 Morantel tartrate Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S5844 Lobelin sulphate Lobelin sulphate (Lobeline sulfate, Bantron) is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation.
S5931 BQCA BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S1405 Vecuronium Bromide Vecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.
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.
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.
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.
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).
S1339 Galanthamine HBr Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
S1397 Rocuronium Bromide Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia.
S1608 Pyridostigmine Bromide Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.
J Am Heart Assoc, 2014, 3(3):e000804
S1832 Atracurium Besylate Atracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.
S1929 Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S2082 Adiphenine HCl Adiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug.
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.
Mol Psychiatry, 2018, 23(3):767-776
S2251 (-)-Huperzine A (HupA) (-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki 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
S2452 Amfebutamone (Bupropion) HCl Amfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
Georgia State University, 2014, Chaquettea Felton
S2462 Donepezil HCl Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
Front Bioeng Biotechnol, 2022, 10:855755
Analyst, 2022, 10.1039/d2an00031h
Front Cardiovasc Med, 2021, 8:639541
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
S3047 Otilonium Bromide Otilonium bromide is an antimuscarinic.
S3202 Catharanthine Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.
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.
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.
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.
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.
S3769 Palmatine Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.
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.
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.
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.
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.
Neurotherapeutics, 2021, 10.1007/s13311-021-01052-3
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.
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.
Acta Pharmacol Sin, 2021, 1-11
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.
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.
S4014 Hyoscyamine Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM.
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 KD of 1.7 μM.
Biomol Ther (Seoul), 2016, 24(5):489-94
Biomol Ther (Seoul), 2016, 24(5):489-94
S4031 Aclidinium Bromide Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.
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.
Front Cell Infect Microbiol, 2021, 11:630812
Am J Cancer Res, 2019, 9(11):2397-2412
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.
S4505 Vinblastine (NSC-49842) sulfate Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Cancer Res, 2021, canres.0955.2021
S4542 Trihexyphenidyl hydrochloride Trihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class.
S4619 Itopride hydrochloride Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
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).
Nature, 2018, 560(7718):372-376
S4776 Harmaline Harmaline, a natural occurrence β-carboline alkaloid, is a central nervous system stimulant and an acetylcholinesterase (AChR) inhibitor; also inhibits histamine N-methyltransferase.
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.
S5022 Varenicline Hydrochloride Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively.
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.
Front Bioeng Biotechnol, 2022, 10:855755
Front Cardiovasc Med, 2021, 8:639541
Int J Pharm, 2019, 560:294-305
S5075 Acotiamide Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
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).
S5424 Carbaryl Carbaryl (1-naphthyl methylcarbamate) is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors.
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
S5511 Ethyl (triphenylphosphoranylidene) acetate Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE.
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.
S5900 Edrophonium chloride Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase.
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.
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.
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.
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
S9179 Catharanthine hemitartrate Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine.
S9219 Huperzine B Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.
S9252 Corydaline Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers.
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.
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).
S4389 Bephenium Hydroxynaphthoate Bephenium 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.
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.
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.
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
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.
S1913 Tropicamide Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.
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
S2054 Orphenadrine Citrate Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.
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.
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S2240 Fesoterodine Fumarate Fesoterodine Fumarate (SPM 907) is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.
Hum Mol Genet, 2020, ddaa244
S2497 Pancuronium dibromide Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant.
Elife, 2019, 8e45399
Front Physiol, 2019, 10:1039
Scholars' Bank, 2019, N/A
S2508 Scopolamine (LSM-4015) HBr Scopolamine HBr (LSM-4015, NSC 61806) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
Exp Ther Med, 2020, 20(4):3625-3632
Mol Cell, 2019, 75(1):53-65
Autophagy, 2019, 10.1080/15548627.2019.1630224
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.
S2549 Trospium chloride Trospium chloride is a competitive muscarinic cholinergic receptor antagonist.
FEBS Lett, 2020, 10.1002/1873-3468.14015
S2550 Tolterodine tartrate Tolterodine tartrate (PNU-200583E) is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist.
JCI Insight, 2019, 4(20)
S2659 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) 5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
S3048 Solifenacin succinate Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class.
S3117 Oxybutynin hydrochloride Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S3144 Darifenacin HBr Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
JCI Insight, 2017, 2(3):e89780
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.
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.
S3735 Umeclidinium bromide Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
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
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.
S4034 Diphemanil Methylsulfate Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).
S4069 Hexamethonium Dibromide Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.
S4143 Pentoxyverine Citrate Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.
S4292 Diphenidol HCl Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.
S4623 Methylbenactyzine Bromide Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity.
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.
S4713 Atropine Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.
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.
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.
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.
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.
S5480 Clidinium Bromide Clidinium Bromide is an anticholinergic drug.
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.
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.
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.
S5873 Scopolamine HBr trihydrate Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
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.
S6469 Thonzylamine Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
S6985New Varenicline Varenicline 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.
E0172New Imidacloprid

Imidacloprid is a nicotinic acetylcholine receptor (nAChR) agonist with potent insecticidal activity.
E0176New 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.
S0717 Varenicline (CP 526555) dihydrochloride Varenicline (CP 526555, Chantix, Champix) 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.
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.
Anticancer Res, 2021, 41(2):687-697
PLoS One, 2019, 14(2):e0211644
Sci Rep, 2016, 6:25705
S1440 Varenicline Tartrate (CP 526555-18) Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction.
S1805 Acetylcholine Chloride The chemical compound Acetylcholine Chloride is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans.
Biotechnol Lett, 2020, 42(7):1219-1227
Med Sci Monit, 2019, 25:5389-5400
S2287 Cytisine Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist.
S2455 Bethanechol chloride Bethanechol chloride 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 is a muscarinic acetylcholine receptor agonist.
Oncogene, 2020, 39(11):2437-2449
BMC Mol Cell Biol, 2020, 21(1):80
Oncol Rep, 2015, 33(6):2753-60
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.
S4072 Decamethonium Bromide Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
S4121 Succinylcholine Chloride Dihydrate Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.
S4171 Choline Chloride Choline chloride 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.
S4231 Pilocarpine HCl Pilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.
Theranostics, 2021, 11(12):5986-6005
Mol Brain, 2021, 14(1):113
Anticancer Res, 2021, 41(2):687-697
S4359 Carbamoylcholine chloride (Carbachol) Carbamoylcholine chloride (Carbachol, Carbamylcholine chloride, Carbastat, Miostat) is a cholinergic agonist that mimics the effect of acetylcholine on both the muscarinic and nicotinic receptors.
S4422 Nitenpyram Nitenpyram 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
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.
Biotechnol Lett, 2020, 42(7):1219-1227
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.
S6432 Cevimeline Cevimeline (AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.
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.
S6887 Clozapine N-oxide Clozapine N-oxide (CNO) 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.
S7366 LY2119620 LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
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.
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.
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) 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 has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
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
Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916
J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR
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.
S3972 Lobeline hydrochloride Lobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors.
J Cell Mol Med, 2020, 10.1111/jcmm.16029
S5747 Morantel tartrate Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S5844 Lobelin sulphate Lobelin sulphate (Lobeline sulfate, Bantron) is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation.
S5931 BQCA BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S6985New Varenicline Varenicline 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.
E0172New Imidacloprid

Imidacloprid is a nicotinic acetylcholine receptor (nAChR) agonist with potent insecticidal activity.
E0176New 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.