AChR

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

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.

S4687New

Rivastigmine

Rivastigmine is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).

S4619New

Itopride hydrochloride

Itopride hydrochloride is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.

S4575New

Pralidoxime chloride

Pralidoxime is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator.

S4542New

Trihexyphenidyl hydrochloride

Trihexyphenidyl hydrochloride is an antiparkinsonian agent of the antimuscarinic class.

S4505New

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.

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.

S4014

Hyoscyamine

Hyoscyamine is an AChR inhibitor with IC50 of 7.5 nM.

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.

S1832

Atracurium Besylate

Atracurium Besylate is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.

S2082

Adiphenine HCl

Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug.

S2629

PNU-120596

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

S4617New

Dextromethorphan hydrobromide hydrate

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

S1405

Vecuronium Bromide

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

S4718New

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.

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

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.

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.

S4660New

Glycopyrrolate

Glycopyrrolate is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.

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.

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.

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 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.

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.

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.

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.

S4069

Hexamethonium Bromide

Hexamethonium Bromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.

S3117

Oxybutynin chloride

Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.

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
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.

S4687New

Rivastigmine

Rivastigmine is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).

S4619New

Itopride hydrochloride

Itopride hydrochloride is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM.

S4575New

Pralidoxime chloride

Pralidoxime is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator.

S4542New

Trihexyphenidyl hydrochloride

Trihexyphenidyl hydrochloride is an antiparkinsonian agent of the antimuscarinic class.

S4505New

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.

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.

S4014

Hyoscyamine

Hyoscyamine is an AChR inhibitor with IC50 of 7.5 nM.

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.

S1832

Atracurium Besylate

Atracurium Besylate is a neuromuscular blocking agent with ED95 of 0.2 mg/kg.

S2082

Adiphenine HCl

Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug.

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.

2014, (84):e51271

S2550

Tolterodine tartrate

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

S4660New

Glycopyrrolate

Glycopyrrolate is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.

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.

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.

2014, 4(6):1081-9

2014, Chaquettea Felton

2014, 10.1534/g3.114.010819

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 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.

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.

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.

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.

S4069

Hexamethonium Bromide

Hexamethonium Bromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.

S3117

Oxybutynin chloride

Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.

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
S4718New

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.

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

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.

Catalog No. Information Product Use Citations Product Validations
S2629

PNU-120596

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

2016, 10.1007/s12035-016-9796-3

2013, 8(8): e73581

Catalog No. Information Product Use Citations Product Validations
S4617New

Dextromethorphan hydrobromide hydrate

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

S1405

Vecuronium Bromide

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