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
S3245^New	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^New	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.
S0016^New	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.
S4357^New	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.
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
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 (ORG 9426) 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 (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
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 (Daturine) 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.
S5886	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.
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).
S4023	Procaine HCl Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with K_D of 1.7 μM.	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	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 ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM.
S3835	Loganin Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively.
S4619	Itopride hydrochloride Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
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.	Am J Cancer Res, 2019, 9(11):2397-2412
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, 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.
S3788	Carvacrol Carvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities.
S9087	Tenuifolin Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production.
S3884	Jatrorrhizine Jatrorrhizine, 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 (NSC49842) 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.	Mol Cancer Ther, 2020, 25;molcanther.1021.2019 Mutagenesis, 2020, 10.1093/mutage/geaa003 Cell Rep, 2020, 32(1):107845
S5075	Acotiamide Acotiamide is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
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.
S3903	Lycorine Lycorine is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis.
S3904	Isoimperatorin Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM.
S9138	Picfeltarraenin IA Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system.
S4542	Trihexyphenidyl hydrochloride Trihexyphenidyl hydrochloride 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.
S5424	Carbaryl Carbaryl is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors.
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.
S9560	Anisodamine Hydrobromide Anisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
S4838	Acotiamide hydrochloride Acotiamide Hydrochloride 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.
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
S4389^New	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 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 (BA 679BR) 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 Appl Physiol (1985), 2018, 125(2):504-512 J Vis Exp, 2014, (84):e51271
S3298^New	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.
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)
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.
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).	Int Forum Allergy Rhinol, 2020, 10(2):233-242 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.	Neurochem Res, 2020, 10.1007/s11064-020-03103-1
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.	Exp Ther Med, 2020, 20(4):3625-3632 Mol Cell, 2019, 75(1):53-65 Autophagy, 2019, 10.1080/15548627.2019.1630224
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.
S5873	Scopolamine HBr trihydrate Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
S4931	Propiverine hydrochloride Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence. Propiverine is a muscarinic receptor antagonist possessing additional properties, i.e., block of L-type Ca2+ channels.
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 (Carbetapentane) 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 (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
S4623	Methylbenactyzine Bromide Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity.
S4069	Hexamethonium Dibromide Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.
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 (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.
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.
S6469	Thonzylamine Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
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.
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.
S1356	Levetiracetam 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.	PLoS One, 2019, 14(2):e0211644 Sci Rep, 2016, 6:25705 Sci Rep, 2016, 6:25705	Levetiracetam reduces DNA, synaptic, and neurite damage caused by Dox. (A) An example of cortical cultures pre-treated with 5 μ M Lev and then Dox (0.01 μ M, overnight), fixed and stained with antibodies against MAP2c. Scale bar is 20 μ m. (B) Cortical neurons at 28–32 DIV were pre-treated with 5 μ M Lev, and then a vehicle or with Dox (0.01 μ M for 3 days, or 0.1 μ M, overnight) was added. Neurons were fixed, and stained for MAP2c, synapsin, and with the Hoechst dye, and imaged. Note that red MAP2c staining also includes Dox's red fluorescence. (C) Synaptically developed primary cortical cultures at 28−32 DIV were pretreated with 5 mM Lev, and then a vehicle or with Dox (0.01 μM for 3 days, or 0.1 μM, overnight) was added. Neurons were then fixed, and stained with antibodies against γH2A.X and MAP2c, and with the Hoechst dye. Blue staining was used by the algorithm to identify and analyze γH2A.X.
S6887^New	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.
S0457^New	DREADD agonist 21 DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.
S6795^New	VU0357017 Hydrochloride VU0357017 hydrochloride 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.
S1440	Varenicline Tartrate Varenicline Tartrate (CP 526555-18) 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.	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 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.	Exp Ther Med, 2020, 20(4):3625-3632 Neurochem Res, 2020, 10.1007/s11064-020-03103-1 Mol Cell, 2019, 75(1):53-65
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.	Proc Natl Acad Sci U S A, 2020, 117(21):11321-11327
S7366	LY2119620 LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
S2287	Cytisine Cytisine (Baphitoxine, Sophorine) 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.
S6432	Cevimeline Cevimeline is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.
S3684	Methacholine chloride Methacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors.
S5930	PNU 282987 HCl PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
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.
S2646^New	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.
S1351	Ivermectin 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.	Nat Cell Biol, 2020, Blood Cancer J, 2020, 10(6):72 Cancers (Basel), 2020, 12(9)E2668
S2629	PNU-120596 PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.	Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916 J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR Mol Pharmacol, 2019, 10.1124/mol.119.116244	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.
S5931	BQCA BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S5844	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.
S5747	Morantel tartrate Morantel is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S1405	Vecuronium Bromide Vecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.
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.
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.

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
S3245^New	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^New	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.
S0016^New	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.
S4357^New	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.
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
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 (ORG 9426) 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 (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
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 (Daturine) 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.
S5886	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.
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).
S4023	Procaine HCl Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with K_D of 1.7 μM.	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	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 ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM.
S3835	Loganin Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively.
S4619	Itopride hydrochloride Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.
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.	Am J Cancer Res, 2019, 9(11):2397-2412
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, 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.
S3788	Carvacrol Carvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities.
S9087	Tenuifolin Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production.
S3884	Jatrorrhizine Jatrorrhizine, 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 (NSC49842) 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.	Mol Cancer Ther, 2020, 25;molcanther.1021.2019 Mutagenesis, 2020, 10.1093/mutage/geaa003 Cell Rep, 2020, 32(1):107845
S5075	Acotiamide Acotiamide is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties.
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.
S3903	Lycorine Lycorine is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis.
S3904	Isoimperatorin Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM.
S9138	Picfeltarraenin IA Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system.
S4542	Trihexyphenidyl hydrochloride Trihexyphenidyl hydrochloride 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.
S5424	Carbaryl Carbaryl is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors.
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.
S9560	Anisodamine Hydrobromide Anisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs).
S4838	Acotiamide hydrochloride Acotiamide Hydrochloride 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.
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

Catalog No.	Information	Product Use Citations	Product Validations
S4389^New	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 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

S4389^New

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 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 (BA 679BR) 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 Appl Physiol (1985), 2018, 125(2):504-512 J Vis Exp, 2014, (84):e51271
S3298^New	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.
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)
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.
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).	Int Forum Allergy Rhinol, 2020, 10(2):233-242 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.	Neurochem Res, 2020, 10.1007/s11064-020-03103-1
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.	Exp Ther Med, 2020, 20(4):3625-3632 Mol Cell, 2019, 75(1):53-65 Autophagy, 2019, 10.1080/15548627.2019.1630224
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.
S5873	Scopolamine HBr trihydrate Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.
S4931	Propiverine hydrochloride Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence. Propiverine is a muscarinic receptor antagonist possessing additional properties, i.e., block of L-type Ca2+ channels.
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 (Carbetapentane) 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 (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
S4623	Methylbenactyzine Bromide Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity.
S4069	Hexamethonium Dibromide Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.
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 (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.
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.
S6469	Thonzylamine Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
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.
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
S1356	Levetiracetam 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.	PLoS One, 2019, 14(2):e0211644 Sci Rep, 2016, 6:25705 Sci Rep, 2016, 6:25705	Levetiracetam reduces DNA, synaptic, and neurite damage caused by Dox. (A) An example of cortical cultures pre-treated with 5 μ M Lev and then Dox (0.01 μ M, overnight), fixed and stained with antibodies against MAP2c. Scale bar is 20 μ m. (B) Cortical neurons at 28–32 DIV were pre-treated with 5 μ M Lev, and then a vehicle or with Dox (0.01 μ M for 3 days, or 0.1 μ M, overnight) was added. Neurons were fixed, and stained for MAP2c, synapsin, and with the Hoechst dye, and imaged. Note that red MAP2c staining also includes Dox's red fluorescence. (C) Synaptically developed primary cortical cultures at 28−32 DIV were pretreated with 5 mM Lev, and then a vehicle or with Dox (0.01 μM for 3 days, or 0.1 μM, overnight) was added. Neurons were then fixed, and stained with antibodies against γH2A.X and MAP2c, and with the Hoechst dye. Blue staining was used by the algorithm to identify and analyze γH2A.X.
S6887^New	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.
S0457^New	DREADD agonist 21 DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.
S6795^New	VU0357017 Hydrochloride VU0357017 hydrochloride 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.
S1440	Varenicline Tartrate Varenicline Tartrate (CP 526555-18) 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.	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 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.	Exp Ther Med, 2020, 20(4):3625-3632 Neurochem Res, 2020, 10.1007/s11064-020-03103-1 Mol Cell, 2019, 75(1):53-65
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.	Proc Natl Acad Sci U S A, 2020, 117(21):11321-11327
S7366	LY2119620 LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
S2287	Cytisine Cytisine (Baphitoxine, Sophorine) 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.
S6432	Cevimeline Cevimeline is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.
S3684	Methacholine chloride Methacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors.
S5930	PNU 282987 HCl PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
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
S2646^New	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.
S1351	Ivermectin 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.	Nat Cell Biol, 2020, Blood Cancer J, 2020, 10(6):72 Cancers (Basel), 2020, 12(9)E2668
S2629	PNU-120596 PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.	Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916 J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR Mol Pharmacol, 2019, 10.1124/mol.119.116244	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.
S5931	BQCA BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
S5844	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.
S5747	Morantel tartrate Morantel is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).

Catalog No.	Information	Product Use Citations	Product Validations
S1405	Vecuronium Bromide Vecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.
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.
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.

Catalog No.

Information

Product Use Citations

Product Validations

S1405

Vecuronium Bromide

Vecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery.

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.

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.