S0016 |
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. |
|
|
S0766 |
RHC 80267
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
|
|
S1339 |
Galanthamine HBr
|
Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. |
|
|
S1397 |
Rocuronium Bromide
|
Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia. |
|
|
S1608 |
Pyridostigmine Bromide
|
Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor. |
-
J Am Heart Assoc, 2014, 3(3):e000804
|
|
S1832 |
Atracurium Besylate
|
Atracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg. |
|
|
S1929 |
Irsogladine
|
Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
|
|
S2082 |
Adiphenine HCl
|
Adiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug. |
|
|
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
|
|
S2251 |
(-)-Huperzine A (HupA)
|
(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4. |
-
Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
|
|
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
|
|
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. |
-
Front Bioeng Biotechnol, 2022, 10:855755
-
Analyst, 2022, 10.1039/d2an00031h
-
Front Cardiovasc Med, 2021, 8:639541
|
|
S2471 |
Gallamine Triethiodide
|
Gallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM. |
-
Mol Cell, 2019, 75(1):53-65
|
|
S2490 |
Neostigmine Bromide
|
Neostigmine Bromide is a reversible acetylcholinesterase inhibitor. |
-
Am J Physiol Gastrointest Liver Physiol, 2016, 310(3):G181-92
|
|
S3047 |
Otilonium Bromide
|
Otilonium bromide is an antimuscarinic. |
|
|
S3202 |
Catharanthine
|
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM. |
|
|
S3245 |
Nodakenetin
|
Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
|
|
S3246 |
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. |
|
|
S3311 |
Myosmine
|
Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM. |
|
|
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 (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
S3866 |
Galanthamine
|
Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders. |
-
Neurotherapeutics, 2021, 10.1007/s13311-021-01052-3
|
|
S3884 |
Jatrorrhizine
|
Jatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
|
|
S3903 |
Lycorine
|
Lycorine (Galanthidine, Amarylline, Narcissine, Licorine, Belamarine) is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis. |
-
Acta Pharmacol Sin, 2021, 1-11
|
|
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. |
|
|
S3913 |
Pimethixene maleate
|
Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. |
|
|
S4014 |
Hyoscyamine
|
Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM. |
|
|
S4023 |
Procaine HCl
|
Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM. |
-
Biomol Ther (Seoul), 2016, 24(5):489-94
-
Biomol Ther (Seoul), 2016, 24(5):489-94
|
|
S4031 |
Aclidinium Bromide
|
Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively. |
|
|
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. |
-
Front Cell Infect Microbiol, 2021, 11:630812
-
Am J Cancer Res, 2019, 9(11):2397-2412
|
|
S4357 |
Tacrine HCl
|
Tacrine is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. |
|
|
S4505 |
Vinblastine (NSC-49842) sulfate
|
Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) 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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
-
Cancer Res, 2021, canres.0955.2021
|
|
S4542 |
Trihexyphenidyl hydrochloride
|
Trihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class. |
|
|
S4619 |
Itopride hydrochloride
|
Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM. |
|
|
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. |
|
|
S4838 |
Acotiamide hydrochloride
|
Acotiamide Hydrochloride (YM-443, Z-338) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor. |
|
|
S5022 |
Varenicline Hydrochloride
|
Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively. |
|
|
S5073 |
Donepezil
|
Donepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type. |
-
Front Bioeng Biotechnol, 2022, 10:855755
-
Front Cardiovasc Med, 2021, 8:639541
-
Int J Pharm, 2019, 560:294-305
|
|
S5075 |
Acotiamide
|
Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties. |
|
|
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). |
|
|
S5424 |
Carbaryl
|
Carbaryl (1-naphthyl methylcarbamate) is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. |
|
|
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
|
|
S5511 |
Ethyl (triphenylphosphoranylidene) acetate
|
Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
|
|
S5886 |
Hodostin
|
Hodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis. |
|
|
S5900 |
Edrophonium chloride
|
Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase. |
|
|
S9069 |
Jatrorrhizine chloride
|
Jatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
|
|
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. |
|
|
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. |
|
|
S9154 |
Chelidonine
|
Chelidonine (Stylophorin, Helidonine), a major bioactive, isoquinoline alkaloid ingredient in Chelidonium majus, exhibits anti-inflammatory properties and acetylcholinesterase and butyrylcholinesterase inhibitory activity. |
-
Onco Targets Ther, 2019, 12:6685-6697
|
|
S9179 |
Catharanthine hemitartrate
|
Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
|
|
S9219 |
Huperzine B
|
Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
|
|
S9252 |
Corydaline
|
Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
|
|
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. |
|
|
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). |
|
|
S4389 |
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 chloride (2-PAM) 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. |
|
|
S0032 |
Batefenterol
|
Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively. |
|
|
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
|
|
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. |
|
|
S1913 |
Tropicamide
|
Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM. |
|
|
S1978 |
Methscopolamine
|
Methscopolamine is a muscarinic acetylcholine receptor blocker. |
-
Mol Brain, 2021, 14(1):113
-
Mol Neurobiol, 2020, 10.1007/s12035-020-02175-y
-
Neuropharmacology, 2019, 146:252-263
|
|
S2054 |
Orphenadrine Citrate
|
Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects. |
|
|
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
|
|
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. |
-
Hum Mol Genet, 2020, ddaa244
|
|
S2497 |
Pancuronium dibromide
|
Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant. |
-
Elife, 2019, 8e45399
-
Front Physiol, 2019, 10:1039
-
Scholars' Bank, 2019, N/A
|
|
S2508 |
Scopolamine (LSM-4015) HBr
|
Scopolamine HBr (LSM-4015, NSC 61806) 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
|
|
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. |
|
|
S2549 |
Trospium chloride
|
Trospium chloride is a competitive muscarinic cholinergic receptor antagonist. |
-
FEBS Lett, 2020, 10.1002/1873-3468.14015
|
|
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)
|
|
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. |
|
|
S3048 |
Solifenacin succinate
|
Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class. |
|
|
S3117 |
Oxybutynin hydrochloride
|
Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties. |
-
Environ Toxicol Chem, 2021, 10.1002/etc.5018
|
|
S3144 |
Darifenacin HBr
|
Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. |
-
JCI Insight, 2017, 2(3):e89780
|
|
S3298 |
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. |
|
|
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.
|
|
|
S3735 |
Umeclidinium bromide
|
Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). |
|
|
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 (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM. |
|
|
S4034 |
Diphemanil Methylsulfate
|
Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR). |
|
|
S4069 |
Hexamethonium Dibromide
|
Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia. |
|
|
S4143 |
Pentoxyverine Citrate
|
Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. |
|
|
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.
|
|
|
S4623 |
Methylbenactyzine Bromide
|
Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity. |
|
|
S4660 |
Glycopyrrolate
|
Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. |
|
|
S4713 |
Atropine
|
Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
|
|
S4834 |
Propantheline bromide
|
Propantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan) is a muscarinic antagonist used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia. |
|
|
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. |
|
|
S4992 |
Nanofin
|
Nanofin (2,6-Dimethylpiperidine, Lupetidine, Naniopinum) is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension. |
|
|
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, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease. |
|
|
S5480 |
Clidinium Bromide
|
Clidinium Bromide is an anticholinergic drug. |
|
|
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. |
|
|
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. |
|
|
S5777 |
Ipratropium bromide monohydrate
|
Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. |
|
|
S5873 |
Scopolamine HBr trihydrate
|
Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
|
|
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. |
|
|
S6469 |
Thonzylamine
|
Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
|
|
S6985New |
Varenicline
|
Varenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. |
|
|
E0172New |
Imidacloprid
|
Imidacloprid is a nicotinic acetylcholine receptor (nAChR) agonist with potent insecticidal activity.
|
|
|
E0176New |
Dinotefuran
|
Dinotefuran (MTI-446), a neonicotinoid, is an effective nAChRs agonist with EC50 of 7.8 μM and shows high insecticidal activity on Da2b2 hybrid nAChRs.
|
|
|
S0457 |
DREADD agonist 21
|
DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM. |
|
|
S0717 |
Varenicline (CP 526555) dihydrochloride
|
Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation. |
|
|
S0720 |
PNU-282987
|
PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM. |
|
|
S1356 |
Levetiracetam (UCB-L059)
|
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. |
-
Anticancer Res, 2021, 41(2):687-697
-
PLoS One, 2019, 14(2):e0211644
-
Sci Rep, 2016, 6:25705
|
|
S1440 |
Varenicline Tartrate (CP 526555-18)
|
Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction. |
|
|
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. |
-
Biotechnol Lett, 2020, 42(7):1219-1227
-
Med Sci Monit, 2019, 25:5389-5400
|
|
S2287 |
Cytisine
|
Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist. |
|
|
S2455 |
Bethanechol chloride
|
Bethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors. |
-
Environ Toxicol Chem, 2021, 10.1002/etc.5018
-
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
-
BMC Mol Cell Biol, 2020, 21(1):80
-
Oncol Rep, 2015, 33(6):2753-60
|
|
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. |
|
|
S4072 |
Decamethonium Bromide
|
Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent. |
|
|
S4121 |
Succinylcholine Chloride Dihydrate
|
Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker. |
|
|
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. |
|
|
S4231 |
Pilocarpine HCl
|
Pilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy. |
-
Theranostics, 2021, 11(12):5986-6005
-
Mol Brain, 2021, 14(1):113
-
Anticancer Res, 2021, 41(2):687-697
|
|
S4359 |
Carbamoylcholine chloride (Carbachol)
|
Carbamoylcholine chloride (Carbachol, Carbamylcholine chloride, Carbastat, Miostat) is a cholinergic agonist that mimics the effect of acetylcholine on both the muscarinic and nicotinic receptors. |
|
|
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
|
|
S4718 |
Acetylcholine iodide
|
Acetylcholine iodide (Acetylcolina) 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. |
-
Biotechnol Lett, 2020, 42(7):1219-1227
|
|
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. |
|
|
S6432 |
Cevimeline
|
Cevimeline (AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3. |
|
|
S6795 |
VU0357017 Hydrochloride
|
VU0357017 hydrochloride (CID-25010775) 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. |
|
|
S6887 |
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. |
|
|
S7366 |
LY2119620
|
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
|
|
|
S9789 |
JHU37152
|
JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
|
|
S9790 |
JHU37160
|
JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
|
|
S0552 |
BNC210
|
BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). |
|
|
S0782 |
VU0238441
|
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively. |
|
|
S0783 |
VU0119498
|
VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively. |
|
|
S1351 |
Ivermectin (MK-933)
|
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. |
-
J Virol, 2021, JVI0148121
-
BMC Cancer, 2021, 21(1):1307
-
Nat Cell Biol, 2020,
|
|
S2629 |
PNU-120596
|
PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM. |
-
Front Med (Lausanne), 2021, 8:642960
-
Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916
-
J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR
|
|
S2646 |
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. |
|
|
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. |
-
J Cell Mol Med, 2020, 10.1111/jcmm.16029
|
|
S5747 |
Morantel tartrate
|
Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs). |
|
|
S5844 |
Lobelin sulphate
|
Lobelin sulphate (Lobeline sulfate, Bantron) is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation. |
|
|
S5931 |
BQCA
|
BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR). |
|
|
S1405 |
Vecuronium Bromide
|
Vecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery. |
|
|
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. |
|
|
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. |
|
|
S0016 |
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. |
|
|
S0766 |
RHC 80267
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
|
|
S1339 |
Galanthamine HBr
|
Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. |
|
|
S1397 |
Rocuronium Bromide
|
Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia. |
|
|
S1608 |
Pyridostigmine Bromide
|
Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor. |
- J Am Heart Assoc, 2014, 3(3):e000804
|
|
S1832 |
Atracurium Besylate
|
Atracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg. |
|
|
S1929 |
Irsogladine
|
Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
|
|
S2082 |
Adiphenine HCl
|
Adiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug. |
|
|
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
|
|
S2251 |
(-)-Huperzine A (HupA)
|
(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4. |
- Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
|
|
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
|
|
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. |
- Front Bioeng Biotechnol, 2022, 10:855755
- Analyst, 2022, 10.1039/d2an00031h
- Front Cardiovasc Med, 2021, 8:639541
|
|
S2471 |
Gallamine Triethiodide
|
Gallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM. |
- Mol Cell, 2019, 75(1):53-65
|
|
S2490 |
Neostigmine Bromide
|
Neostigmine Bromide is a reversible acetylcholinesterase inhibitor. |
- Am J Physiol Gastrointest Liver Physiol, 2016, 310(3):G181-92
|
|
S3047 |
Otilonium Bromide
|
Otilonium bromide is an antimuscarinic. |
|
|
S3202 |
Catharanthine
|
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM. |
|
|
S3245 |
Nodakenetin
|
Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
|
|
S3246 |
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. |
|
|
S3311 |
Myosmine
|
Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM. |
|
|
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 (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
S3866 |
Galanthamine
|
Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders. |
- Neurotherapeutics, 2021, 10.1007/s13311-021-01052-3
|
|
S3884 |
Jatrorrhizine
|
Jatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
|
|
S3903 |
Lycorine
|
Lycorine (Galanthidine, Amarylline, Narcissine, Licorine, Belamarine) is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis. |
- Acta Pharmacol Sin, 2021, 1-11
|
|
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. |
|
|
S3913 |
Pimethixene maleate
|
Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. |
|
|
S4014 |
Hyoscyamine
|
Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM. |
|
|
S4023 |
Procaine HCl
|
Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM. |
- Biomol Ther (Seoul), 2016, 24(5):489-94
- Biomol Ther (Seoul), 2016, 24(5):489-94
|
|
S4031 |
Aclidinium Bromide
|
Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively. |
|
|
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. |
- Front Cell Infect Microbiol, 2021, 11:630812
- Am J Cancer Res, 2019, 9(11):2397-2412
|
|
S4357 |
Tacrine HCl
|
Tacrine is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. |
|
|
S4505 |
Vinblastine (NSC-49842) sulfate
|
Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) 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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
- Cancer Res, 2021, canres.0955.2021
|
|
S4542 |
Trihexyphenidyl hydrochloride
|
Trihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class. |
|
|
S4619 |
Itopride hydrochloride
|
Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM. |
|
|
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. |
|
|
S4838 |
Acotiamide hydrochloride
|
Acotiamide Hydrochloride (YM-443, Z-338) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor. |
|
|
S5022 |
Varenicline Hydrochloride
|
Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively. |
|
|
S5073 |
Donepezil
|
Donepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type. |
- Front Bioeng Biotechnol, 2022, 10:855755
- Front Cardiovasc Med, 2021, 8:639541
- Int J Pharm, 2019, 560:294-305
|
|
S5075 |
Acotiamide
|
Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties. |
|
|
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). |
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S5424 |
Carbaryl
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Carbaryl (1-naphthyl methylcarbamate) is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. |
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S5493 |
Atropine sulfate
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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
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S5511 |
Ethyl (triphenylphosphoranylidene) acetate
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Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
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S5886 |
Hodostin
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Hodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis. |
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S5900 |
Edrophonium chloride
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Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase. |
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S9069 |
Jatrorrhizine chloride
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Jatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
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S9087 |
Tenuifolin
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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. |
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S9138 |
Picfeltarraenin IA
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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. |
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S9154 |
Chelidonine
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Chelidonine (Stylophorin, Helidonine), a major bioactive, isoquinoline alkaloid ingredient in Chelidonium majus, exhibits anti-inflammatory properties and acetylcholinesterase and butyrylcholinesterase inhibitory activity. |
- Onco Targets Ther, 2019, 12:6685-6697
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S9179 |
Catharanthine hemitartrate
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Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
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S9219 |
Huperzine B
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Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
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S9252 |
Corydaline
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Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
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S9260 |
Nodakenin
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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. |
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S9560 |
Anisodamine Hydrobromide
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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). |
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S0032 |
Batefenterol
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Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively. |
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S1683 |
Ipratropium Bromide
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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
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S1754 |
Oxybutynin
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Oxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties. |
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S1913 |
Tropicamide
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Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM. |
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S1978 |
Methscopolamine
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Methscopolamine is a muscarinic acetylcholine receptor blocker. |
- Mol Brain, 2021, 14(1):113
- Mol Neurobiol, 2020, 10.1007/s12035-020-02175-y
- Neuropharmacology, 2019, 146:252-263
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S2054 |
Orphenadrine Citrate
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Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects. |
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S2130 |
Atropine sulfate monohydrate
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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
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S2240 |
Fesoterodine Fumarate
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Fesoterodine Fumarate (SPM 907) is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome. |
- Hum Mol Genet, 2020, ddaa244
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S2497 |
Pancuronium dibromide
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Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant. |
- Elife, 2019, 8e45399
- Front Physiol, 2019, 10:1039
- Scholars' Bank, 2019, N/A
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S2508 |
Scopolamine (LSM-4015) HBr
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Scopolamine HBr (LSM-4015, NSC 61806) 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
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S2547 |
Tiotropium Bromide hydrate
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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. |
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S2549 |
Trospium chloride
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Trospium chloride is a competitive muscarinic cholinergic receptor antagonist. |
- FEBS Lett, 2020, 10.1002/1873-3468.14015
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S2550 |
Tolterodine tartrate
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Tolterodine tartrate (PNU-200583E) is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist. |
- JCI Insight, 2019, 4(20)
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S2659 |
5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)
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5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM. |
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S3048 |
Solifenacin succinate
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Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class. |
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S3117 |
Oxybutynin hydrochloride
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Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties. |
- Environ Toxicol Chem, 2021, 10.1002/etc.5018
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S3144 |
Darifenacin HBr
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Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. |
- JCI Insight, 2017, 2(3):e89780
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S3298 |
Caulophylline (N-Methylcytisine)
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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. |
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S3701 |
Benactyzine hydrochloride
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Benactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety.
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S3735 |
Umeclidinium bromide
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Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). |
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S4024 |
Homatropine Methylbromide
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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
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S4025 |
Homatropine Bromide
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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. |
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S4027 |
Flavoxate HCl
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Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM. |
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S4034 |
Diphemanil Methylsulfate
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Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR). |
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S4069 |
Hexamethonium Dibromide
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Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia. |
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S4143 |
Pentoxyverine Citrate
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Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. |
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S4292 |
Diphenidol HCl
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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.
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S4623 |
Methylbenactyzine Bromide
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Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity. |
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S4660 |
Glycopyrrolate
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Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. |
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S4713 |
Atropine
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Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
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S4834 |
Propantheline bromide
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Propantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan) is a muscarinic antagonist used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia. |
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S4931 |
Propiverine hydrochloride
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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. |
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S4992 |
Nanofin
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Nanofin (2,6-Dimethylpiperidine, Lupetidine, Naniopinum) is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension. |
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S5238 |
Solifenacin (YM905)
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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. |
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S5258 |
Revefenacin
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Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease. |
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S5480 |
Clidinium Bromide
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Clidinium Bromide is an anticholinergic drug. |
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S5538 |
Tropisetron
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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. |
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S5699 |
Scopolamine N-Oxide HydrobroMide Monohydrate
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Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. |
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S5777 |
Ipratropium bromide monohydrate
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Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. |
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S5873 |
Scopolamine HBr trihydrate
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Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
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S5921 |
Cyclopentolate Hydrochloride
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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. |
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S6469 |
Thonzylamine
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Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
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S6985New |
Varenicline
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Varenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. |
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