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AChR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
Verified customer review of Donepezil HCl
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
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
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
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
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
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
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
S1397 Rocuronium Bromide Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia.
Cureus, 2024, 16(12):e76537
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
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
S4542 Trihexyphenidyl hydrochloride Trihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class.
Cell Commun Signal, 2024, 22(1):551
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
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 Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.
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). This compound 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. This compound 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 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. This compound 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.
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.
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. This compound has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM.
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, antimutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities.
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), a salt of vasicine (VAS), is a potential natural cholinesterase inhibitor. This alkaloid, isolated from Adhatoda vasica, 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. This compound 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.
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.
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.
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.
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. This compound induces autophagy and apoptosis.
Biomed Pharmacother, 2025, 188:118203
Int J Mol Sci, 2025, 26(8)3864
J Mol Cell Biol, 2025, mjaf023
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
Verified customer review of Procaine HCl
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
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.
CNS Neurosci Ther, 2025, 31(8):e70588
S1929 Irsogladine Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
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). This compound alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. It exhibits anti-tumor activity.
S3835 Loganin Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. This compound 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.
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.
S0016 SN-6 SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. This compound inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. It 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).