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.

S2251

(-)-Huperzine A (HupA)

(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.

S4357New

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.

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 Ki 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.

S1608

Pyridostigmine Bromide

Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.

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.

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.

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.

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 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 is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.

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.

S3788

Carvacrol

Carvacrol, 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 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.

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).

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.

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 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 is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects.

S4389New

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 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.

S2550

Tolterodine tartrate

Tolterodine tartrate is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist.

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).

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.

S2659

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

S3144

Darifenacin HBr

Darifenacin is a selective M3 muscarinic receptor antagonist with pKi 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.

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.

S6469

Thonzylamine

Thonzylamine 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 pKb 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.

S6795New

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 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.

S2614

Arecoline HBr

Arecoline is a muscarinic acetylcholine receptor agonist.

S4231

Pilocarpine HCl

Pilocarpine HCl is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.

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.

S6432

Cevimeline

Cevimeline is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.

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.

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.

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.

S2646New

VU0238429

VU0238429 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.

S2629

PNU-120596

PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

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 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 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 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.

S2251

(-)-Huperzine A (HupA)

(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.

S4357New

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.

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 Ki 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.

S1608

Pyridostigmine Bromide

Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.

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.

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.

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.

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 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 is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.

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.

S3788

Carvacrol

Carvacrol, 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 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.

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).

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.

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 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 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
S4389New

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
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.

S2550

Tolterodine tartrate

Tolterodine tartrate is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist.

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).

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.

S2659

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

S3144

Darifenacin HBr

Darifenacin is a selective M3 muscarinic receptor antagonist with pKi 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.

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.

S6469

Thonzylamine

Thonzylamine 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 pKb 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
S6795New

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 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.

S2614

Arecoline HBr

Arecoline is a muscarinic acetylcholine receptor agonist.

S4231

Pilocarpine HCl

Pilocarpine HCl is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.

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.

S6432

Cevimeline

Cevimeline is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.

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.

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.

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
S2646New

VU0238429

VU0238429 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.

S2629

PNU-120596

PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

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 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 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 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.