AChR

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

AChR Products

Catalog No.	Information	Product Use Citations	Product Validations
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.	Anticancer Res, 2018, 38(9):5149-5157 Mol Psychiatry, 2018, 23(3):767-776 Anal Bioanal Chem, 2017, 409(28):6635-6642	Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
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
S5886^New	Hodostin Hodostin is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis.
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.	G3 (Bethesda), 2014, 4(6):1081-9 Georgia State University, 2014, Chaquettea Felton G3 (Bethesda), 2014, 10.1534/g3.114.010819
S1339	Galanthamine HBr Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
S4031	Aclidinium Bromide Aclidinium Bromide 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 is a competitive AchR antagonist, used in modern anaesthesia.
S3047	Otilonium Bromide Otilonium bromide is an antimuscarinic.
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
S1608	Pyridostigmine Bromide Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.	J Am Heart Assoc, 2014, 3(3):e000804	Acetylcholine (ACh)-related protein expression in vivo. Choline acetyltransferase (ChAT) in the ischemic area were determined among 3 experimental groups. Data of Western blotting are represented as fold of control.
S2087	Rivastigmine Tartrate Rivastigmine Tartrate 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
S1929	Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S2490	Neostigmine Bromide Neostigmine Bromide is a reversible acetylcholinesterase inhibitor.
S3202	Catharanthine Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.
S5073	Donepezil Donepezil 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.	Int J Pharm, 2019, 560:294-305
S4014	Hyoscyamine Hyoscyamine is an AChR inhibitor with IC50 of 7.5 nM.
S9219	Huperzine B Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.
S4023	Procaine HCl Procaine 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	Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. p<0.05, *p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
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.
S5900	Edrophonium chloride Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase.
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 is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.
S9260	Nodakenin Nodakenin, 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 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 is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
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.
S3639	Tacrine hydrochloride hydrate Tacrine 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, an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.
s9069	Jatrorrhizine chloride Jatrorrhizine chloride 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.
S3884	Jatrorrhizine Jatrorrhizine, 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.
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.	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 Nucleic Acids Res, 2019, 10.1093/nar/gkz602
S5075	Acotiamide Acotiamide is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
S4687	Rivastigmine Rivastigmine 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.
S3903	Lycorine Lycorine is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis.
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 is an antiparkinsonian agent of the antimuscarinic class.
S5511	Ethyl (triphenylphosphoranylidene) acetate Ethyl (triphenylphosphoranylidene) acetate may act as an inhibitor of cholinesterase that inhibits AChE and BChE.
S2082	Adiphenine HCl Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug.
S9154	Chelidonine Chelidonine, 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 Galantamine 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 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.
S5493	Atropine sulfate Atropine Sulfate is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects.
S4575	Pralidoxime chloride Pralidoxime 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.
S2547	Tiotropium Bromide hydrate Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.
S2497	Pancuronium dibromide Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant.	J Vis Exp, 2014, (84):e51271
S2550	Tolterodine tartrate Tolterodine tartrate is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist.
S5921^New	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^New	Thonzylamine Thonzylamine is an antihistamine and anticholinergic drug.
S5873^New	Scopolamine HBr trihydrate Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
S2240	Fesoterodine Fumarate Fesoterodine Fumarate is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.
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 is a urinary antispasmodic of the antimuscarinic class.
S1683	Ipratropium Bromide Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD).	Anal Chem, 2019, 91(18):11888-11896
S2549	Trospium chloride Trospium chloride is a competitive muscarinic cholinergic receptor antagonist.
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.
S1978	Methscopolamine Methscopolamine is a muscarinic acetylcholine receptor blocker.
S2508	Scopolamine HBr Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.	Mol Cell, 2019, 75(1):53-65 Autophagy, 2019, 10.1080/15548627.2019.1630224 Nature, 2018, 560(7718):372-376
S2659	5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) 5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with K_b of 0.84 nM.
S3144	Darifenacin HBr Darifenacin is a selective M3 muscarinic receptor antagonist with pK_i of 8.9.
S5480	Clidinium Bromide Clidinium Bromide is an anticholinergic drug.
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 is a muscarinic AChR antagonist with IC50 of 12.2 μM.
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) 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).
S4143	Pentoxyverine Citrate Pentoxyverine Citrate is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.
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 is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
S4623	Methylbenactyzine Bromide Methylbenactyzine Bromide 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.
S4660	Glycopyrrolate Glycopyrrolate is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.
S3735	Umeclidinium bromide Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
S5538	Tropisetron Tropisetron is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
S3117	Oxybutynin hydrochloride Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.
S4834	Propantheline bromide
S4992	Nanofin Nanofin is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension.
S4292	Diphenidol HCl Diphenidol HCl 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 is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.
S6432^New	Cevimeline Cevimeline is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.
S5930^New	PNU 282987 PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
S1440	Varenicline Tartrate Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.
S2455	Bethanechol chloride Bethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors.	Lung, 2018, 196(2):219-229
S2614	Arecoline HBr Arecoline is a muscarinic acetylcholine receptor agonist.	Oncol Rep, 2015, 33(6):2753-60	Arecoline affects expression of epithelial-mesenchymal transition-related genes in a dose-dependent manner. Expression of epithelial-mesenchymal transition-related genes (CK19, E-cadherin, N-cadherin and vimentin) in HaCaT cells was determined by western blotting and the results were quantified. Data shown are means ± SD, P<0.05, P<0.01, **P<0.001. CK19, cytokeratin 19.
S4231	Pilocarpine HCl Pilocarpine HCl is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.	Mol Cell, 2019, 75(1):53-65 Autophagy, 2019, 10.1080/15548627.2019.1630224
S4121	Succinylcholine Chloride Dihydrate Succinylcholine Chloride Dihydrate is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.
S4422	Nitenpyram Nitenpyram is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.
S7366	LY2119620 LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
S2287	Cytisine Cytisine is a nicotinic acetylcholine receptor agonist.
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.
S4072	Decamethonium Bromide Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
S3684	Methacholine chloride Methacholine 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.
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.	Med Sci Monit, 2019, 25:5389-5400
S4718	Acetylcholine iodide Acetylcholine iodide 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.
S5844^New	Lobelin sulphate Lobelin sulphate 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^New	BQCA BQCA is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S2629	PNU-120596 PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.	Mol Pharmacol, 2019, 10.1124/mol.119.116244 Mol Neurobiol, 2017, 54(3):2045-2059 Mol Neurobiol, 2016, 10.1007/s12035-016-9796-3	C) A summary: MCAO-induced infarct volumes were significantly smaller in treated vs. untreated animals: p=0.0147 (n=10; two-tailed, the Mann–Whitney U-test). The results are presented as mean+S.E.M.
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.
S5747	Morantel tartrate Morantel is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S9560^New	Anisodamine Hydrobromide Anisodamine is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
S1405	Vecuronium Bromide Vecuronium is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.
S4617	Dextromethorphan hydrobromide hydrate Dextromethorphan is an antitussive (cough suppressant) drug of the morphinan class with sedative, dissociative, and stimulant properties (at higher doses).

Catalog No.	Information	Product Use Citations	Product Validations
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.	Anticancer Res, 2018, 38(9):5149-5157 Mol Psychiatry, 2018, 23(3):767-776 Anal Bioanal Chem, 2017, 409(28):6635-6642	Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
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
S5886^New	Hodostin Hodostin is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis.
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.	G3 (Bethesda), 2014, 4(6):1081-9 Georgia State University, 2014, Chaquettea Felton G3 (Bethesda), 2014, 10.1534/g3.114.010819
S1339	Galanthamine HBr Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
S4031	Aclidinium Bromide Aclidinium Bromide 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 is a competitive AchR antagonist, used in modern anaesthesia.
S3047	Otilonium Bromide Otilonium bromide is an antimuscarinic.
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
S1608	Pyridostigmine Bromide Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.	J Am Heart Assoc, 2014, 3(3):e000804	Acetylcholine (ACh)-related protein expression in vivo. Choline acetyltransferase (ChAT) in the ischemic area were determined among 3 experimental groups. Data of Western blotting are represented as fold of control.
S2087	Rivastigmine Tartrate Rivastigmine Tartrate 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
S1929	Irsogladine Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
S2490	Neostigmine Bromide Neostigmine Bromide is a reversible acetylcholinesterase inhibitor.
S3202	Catharanthine Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.
S5073	Donepezil Donepezil 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.	Int J Pharm, 2019, 560:294-305
S4014	Hyoscyamine Hyoscyamine is an AChR inhibitor with IC50 of 7.5 nM.
S9219	Huperzine B Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.
S4023	Procaine HCl Procaine 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	Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. p<0.05, *p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
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.
S5900	Edrophonium chloride Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase.
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 is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.
S9260	Nodakenin Nodakenin, 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 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 is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
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.
S3639	Tacrine hydrochloride hydrate Tacrine 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, an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.
s9069	Jatrorrhizine chloride Jatrorrhizine chloride 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.
S3884	Jatrorrhizine Jatrorrhizine, 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.
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.	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 Nucleic Acids Res, 2019, 10.1093/nar/gkz602
S5075	Acotiamide Acotiamide is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
S4687	Rivastigmine Rivastigmine 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.
S3903	Lycorine Lycorine is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis.
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 is an antiparkinsonian agent of the antimuscarinic class.
S5511	Ethyl (triphenylphosphoranylidene) acetate Ethyl (triphenylphosphoranylidene) acetate may act as an inhibitor of cholinesterase that inhibits AChE and BChE.
S2082	Adiphenine HCl Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug.
S9154	Chelidonine Chelidonine, 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 Galantamine 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 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.
S5493	Atropine sulfate Atropine Sulfate is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects.

Catalog No.	Information	Product Use Citations	Product Validations
S4575	Pralidoxime chloride Pralidoxime 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.

Catalog No.

Information

Product Use Citations

Product Validations

S4575

Pralidoxime chloride

Pralidoxime 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.

Catalog No.	Information	Product Use Citations
S2547	Tiotropium Bromide hydrate Tiotropium Bromide hydrate is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist.
S2497	Pancuronium dibromide Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant.	J Vis Exp, 2014, (84):e51271
S2550	Tolterodine tartrate Tolterodine tartrate is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist.
S5921^New	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^New	Thonzylamine Thonzylamine is an antihistamine and anticholinergic drug.
S5873^New	Scopolamine HBr trihydrate Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
S2240	Fesoterodine Fumarate Fesoterodine Fumarate is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome.
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 is a urinary antispasmodic of the antimuscarinic class.
S1683	Ipratropium Bromide Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD).	Anal Chem, 2019, 91(18):11888-11896
S2549	Trospium chloride Trospium chloride is a competitive muscarinic cholinergic receptor antagonist.
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.
S1978	Methscopolamine Methscopolamine is a muscarinic acetylcholine receptor blocker.
S2508	Scopolamine HBr Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.	Mol Cell, 2019, 75(1):53-65 Autophagy, 2019, 10.1080/15548627.2019.1630224 Nature, 2018, 560(7718):372-376
S2659	5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) 5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with K_b of 0.84 nM.
S3144	Darifenacin HBr Darifenacin is a selective M3 muscarinic receptor antagonist with pK_i of 8.9.
S5480	Clidinium Bromide Clidinium Bromide is an anticholinergic drug.
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 is a muscarinic AChR antagonist with IC50 of 12.2 μM.
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) 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).
S4143	Pentoxyverine Citrate Pentoxyverine Citrate is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.
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 is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
S4623	Methylbenactyzine Bromide Methylbenactyzine Bromide 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.
S4660	Glycopyrrolate Glycopyrrolate is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.
S3735	Umeclidinium bromide Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
S5538	Tropisetron Tropisetron is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
S3117	Oxybutynin hydrochloride Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.
S4834	Propantheline bromide
S4992	Nanofin Nanofin is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension.
S4292	Diphenidol HCl Diphenidol HCl 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 is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.

Catalog No.	Information	Product Use Citations	Product Validations
S6432^New	Cevimeline Cevimeline is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.
S5930^New	PNU 282987 PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
S1440	Varenicline Tartrate Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.
S2455	Bethanechol chloride Bethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors.	Lung, 2018, 196(2):219-229
S2614	Arecoline HBr Arecoline is a muscarinic acetylcholine receptor agonist.	Oncol Rep, 2015, 33(6):2753-60	Arecoline affects expression of epithelial-mesenchymal transition-related genes in a dose-dependent manner. Expression of epithelial-mesenchymal transition-related genes (CK19, E-cadherin, N-cadherin and vimentin) in HaCaT cells was determined by western blotting and the results were quantified. Data shown are means ± SD, P<0.05, P<0.01, **P<0.001. CK19, cytokeratin 19.
S4231	Pilocarpine HCl Pilocarpine HCl is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.	Mol Cell, 2019, 75(1):53-65 Autophagy, 2019, 10.1080/15548627.2019.1630224
S4121	Succinylcholine Chloride Dihydrate Succinylcholine Chloride Dihydrate is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.
S4422	Nitenpyram Nitenpyram is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.
S7366	LY2119620 LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
S2287	Cytisine Cytisine is a nicotinic acetylcholine receptor agonist.
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.
S4072	Decamethonium Bromide Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
S3684	Methacholine chloride Methacholine 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.
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.	Med Sci Monit, 2019, 25:5389-5400
S4718	Acetylcholine iodide Acetylcholine iodide 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.

Catalog No.	Information	Product Use Citations	Product Validations
S5844^New	Lobelin sulphate Lobelin sulphate 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^New	BQCA BQCA is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S2629	PNU-120596 PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.	Mol Pharmacol, 2019, 10.1124/mol.119.116244 Mol Neurobiol, 2017, 54(3):2045-2059 Mol Neurobiol, 2016, 10.1007/s12035-016-9796-3	C) A summary: MCAO-induced infarct volumes were significantly smaller in treated vs. untreated animals: p=0.0147 (n=10; two-tailed, the Mann–Whitney U-test). The results are presented as mean+S.E.M.
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.
S5747	Morantel tartrate Morantel is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).

Catalog No.	Information	Product Use Citations	Product Validations
S9560^New	Anisodamine Hydrobromide Anisodamine is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
S1405	Vecuronium Bromide Vecuronium is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.
S4617	Dextromethorphan hydrobromide hydrate Dextromethorphan is an antitussive (cough suppressant) drug of the morphinan class with sedative, dissociative, and stimulant properties (at higher doses).

Catalog No.

Information

Product Use Citations

Product Validations

S9560^New

Anisodamine Hydrobromide

Anisodamine is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).

S1405

Vecuronium Bromide

Vecuronium is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.

S4617

Dextromethorphan hydrobromide hydrate

Dextromethorphan is an antitussive (cough suppressant) drug of the morphinan class with sedative, dissociative, and stimulant properties (at higher doses).