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. Vinblastine sulfate induces autophagy and apoptosis. |
-
Nat Commun, 2023, 14(1):7576
-
J Immunother Cancer, 2023, 11(8)e007253
-
J Immunother Cancer, 2023, 10.1136/jitc-2023-007253
|
|
S1351 |
Ivermectin
|
Ivermectin 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 (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
-
Viruses, 2024, 16(4)640
-
Life Sci Alliance, 2023, 6(8)e202302133
-
Cell Rep Methods, 2023, 3(10):100599
|
|
S2462 |
Donepezil HCl
|
Donepezil HCl is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration. |
-
Theranostics, 2023, 13(6):1826-1842
-
J Cell Physiol, 2023, 10.1002/jcp.31057
-
Comp Biochem Physiol C Toxicol Pharmacol, 2023, 272:109698
|
|
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
-
J Leukoc Biol, 2020, 10.1002/JLB.6MA0720-344RRR
-
Pharmacol Biochem Behav, 2020, 10.1016/j.pbb.2020.172916
|
|
S4231 |
Pilocarpine HCl
|
Pilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy. |
-
Heliyon, 2024, 10(1):e23945
-
Theranostics, 2021, 11(12):5986-6005
-
Mol Brain, 2021, 14(1):113
|
|
S2497 |
Pancuronium dibromide
|
Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant. |
-
bioRxiv, 2024, 2024.05.23.595327
-
Biomedicines, 2022, 10(12)3056
-
Elife, 2019, 8e45399
|
|
S2508 |
Scopolamine (LSM-4015) HBr
|
Scopolamine HBr (LSM-4015,NSC 61806,(-)-Scopolamine hydrobromide, Hyoscine hydrobromide, Scopine hydrobromide) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
-
Heliyon, 2024, 10(1):e23945
-
Zool Res, 2023, 44(4):712-724
-
Zool Res, 2023, 44(4):712-724
|
|
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. |
-
Nat Commun, 2023, 10.1038/s41467-023-42332-0
-
Nat Commun, 2023, 14(1):6690
-
iScience, 2023, 26(8):107477
|
|
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. |
-
Front Neurosci, 2023, 17:1336026
-
bioRxiv, 2023, 2023.11.10.566574
-
Alzheimers Dement (N Y), 2022, 8(1):e12329
|
|
S6887 |
CNO (Clozapine N-oxide)
|
CNO (Clozapine N-oxide) 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.Solutions are unstable and should be fresh-prepared. |
-
Theranostics, 2024, 14(7):2881-2896
-
Theranostics, 2024, 14(7):2881-2896
-
Cell Rep, 2024, 43(8):114529
|
|
S2452 |
Amfebutamone (Bupropion) HCl
|
Amfebutamone (Bupropion) HCl(Wellbutrin) 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
-
G3 (Bethesda), 2014, 10.1534/g3.114.010819
|
|
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. |
-
Theranostics, 2023, 13(6):1826-1842
-
Front Bioeng Biotechnol, 2022, 10:855755
-
Front Cardiovasc Med, 2021, 8:639541
|
|
S1805 |
Acetylcholine Chloride
|
The chemical compound Acetylcholine Chloride(ACh chloride) is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans. |
-
Cell Mol Life Sci, 2024, 81(1):88
-
iScience, 2023, 26(3):106241
-
Cell, 2022, 185-21:3950-3965.e25
|
|
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
|
|
S2455 |
Bethanechol chloride
|
Bethanechol chloride(Myocholine,Urecholine) 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(NSC-31750) is a muscarinic acetylcholine receptor agonist. |
-
Antioxidants (Basel), 2024, 13(4)430
-
Int J Oral Sci, 2024, 16(1):17
-
Oncogene, 2020, 39(11):2437-2449
|
|
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
|
|
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. |
-
Neurosci Bull, 2023, none
-
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
|
|
S3047 |
Otilonium Bromide
|
Otilonium bromide is an antimuscarinic. |
-
Biochem Pharmacol, 2023, 215:115746
-
Res Microbiol, 2022, S0923-2508(22)00073-0
|
|
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. |
-
J Cell Physiol, 2023, 10.1002/jcp.31057
-
Mol Psychiatry, 2018, 23(3):767-776
|
|
S3144 |
Darifenacin HBr
|
Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. |
-
AAPS PharmSciTech, 2024, 25(7):204
-
World J Gastroenterol, 2023, 29(20):3103-3118
-
JCI Insight, 2017, 2(3):e89780
|
|
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
|
|
S4171 |
Choline Chloride
|
Choline chloride(Hepacholine) 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. |
-
Nat Commun, 2023, 14(1):5034
-
Nat Commun, 2023, 14(1):5034
|
|
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. |
-
Kaohsiung J Med Sci, 2023, none
-
Acta Pharmacol Sin, 2021, 1-11
|
|
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. |
-
Food Sci Nutr, 2022, 10(8):2773-2785
-
Biotechnol Lett, 2020, 42(7):1219-1227
|
|
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
|
|
S1440 |
Varenicline Tartrate (CP 526555-18)
|
Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction. |
-
Neuropharmacology, 2023, S0028-3908(23)00262-9
|
|
S1339 |
Galanthamine HBr
|
Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. |
-
J Cell Physiol, 2023, 10.1002/jcp.31057
|
|
S2549 |
Trospium chloride
|
Trospium chloride is a competitive muscarinic cholinergic receptor antagonist. |
-
FEBS Lett, 2020, 10.1002/1873-3468.14015
|
|
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
|
|
S4014 |
Hyoscyamine
|
Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM. |
-
Theranostics, 2022, 12(12):5488-5503
|
|
S4713 |
Atropine
|
Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
-
iScience, 2023, 26(3):106241
|
|
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
|
|
S4121 |
Succinylcholine Chloride Dihydrate
|
Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker. |
-
Cell Rep Methods, 2023, 3(10):100599
|
|
S5900 |
Edrophonium chloride
|
Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase. |
-
Int J Mol Sci, 2023, 10.3390/ijms242115535
|
|
S4422 |
Nitenpyram
|
Nitenpyram(Bestguard,Capstar) 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
|
|
S2287 |
Cytisine
|
Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist. |
-
Transl Oncol, 2023, 35:101712
|
|
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. |
-
J Clin Med, 2022, 11(9)2307
|
|
S6432 |
Cevimeline HCl hemihydrate
|
Cevimeline HCl hemihydrate(AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3. |
-
Front Pharmacol, 2022, 13:914153
|
|
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
|
|
S3117 |
Oxybutynin hydrochloride
|
Oxybutynin(MJ4309-1) is an anticholinergic medication used to relieve urinary and bladder difficulties. |
-
Environ Toxicol Chem, 2021, 10.1002/etc.5018
|
|
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
|
|
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. |
|
|
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
|
|
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. |
|
|
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 (YM905) is a urinary antispasmodic of the antimuscarinic class. |
|
|
S1405 |
Vecuronium Bromide
|
Vecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery. |
|
|
S2378 |
Butylscopolamine Bromide
|
Butylscopolamine Bromide (Scopolamine Butylbromide,(-)-Scopolamine butylbromide, Hyoscine butylbromide), is a peripherally acting antimuscarinic, anticholinergic agent used as an abdominal-specific antispasmodic. |
|
|
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. |
|
|
S1397 |
Rocuronium Bromide
|
Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia. |
|
|
S1929 |
Irsogladine
|
Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
|
|
E0524 |
Spinosad
|
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete, is a biological neurotoxic insecticide with a broader action spectrum, targeting the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. |
|
|
S5873 |
Scopolamine HBr trihydrate
|
Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
|
|
S3202 |
Catharanthine
|
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM. |
|
|
S0717 |
Varenicline (CP 526555) dihydrochloride
|
Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) 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. |
|
|
S4575 |
Pralidoxime chloride
|
Pralidoxime chloride (2-PAM) is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
S0518 |
NS 1738
|
NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nicotinic acetylcholine receptor (α7 nAChR), with respect to positive modulation of Xenopus laevis oocyte α7 nAChR with EC50 of 3.4 μM, as well as a comparable efficacy at the rat α7 nAChR with EC50 of 3.9 μM. |
|
|
E3551 |
Stephania Extract
|
Stephania Extract is extracted from Stephania, which ameliorates Scopolamine-Induced Memory Impairment in Mice through Inhibition of Acetylcholinesterase and Oxidative Stress. |
|
|
S9219 |
Huperzine B
|
Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
|
|
S0521 |
PNU-282987 S enantiomer free base
|
PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base, which is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
S5480 |
Clidinium Bromide
|
Clidinium Bromide(Ro 2-3773) is an anticholinergic drug. |
|
|
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). |
|
|
S6985 |
Varenicline
|
Varenicline(CP 526555) 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. |
|
|
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. |
|
|
E4822New |
Tacrine
|
Tacrine is a potent acetylcholinesterase (AChE) inhibitor. It inhibits acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) with an IC50 of 77 nM and 69 nM, respectively. It is used in the treatment of Alzheimer's disease (AD), also poisoning topoisomerases and inhibiting in vivo (mitochondrial)mtDNA synthesis. |
|
|
S4027 |
Flavoxate HCl
|
Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM. |
|
|
S9326 |
Scopolamine
|
Scopolamine (Skopolamin) is a tropane alkaloid derived from plants of the nightshade family, specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties. |
-
Immunity, 2024, 57(2):364-378.e9
|
|
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. |
|
|
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. |
|
|
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. |
|
|
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). |
|
|
E3651 |
Lycopodiastrum casuarinoides Extract
|
Lycopodiastrum casuarinoides Extract is extracted from Lycopodiastrum casuarinoides, which has acetylcholinesterase inhibitory activity. |
|
|
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 (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg. |
|
|
S0552 |
BNC210
|
BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). |
|
|
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). |
|
|
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. |
|
|
S5022 |
Varenicline Hydrochloride
|
Varenicline (CP 526555) Hydrochloride is a partial agonist of α4β2 nicotine acetylcholine receptor (nAChR) and α6β2 nicotine acetylcholine receptor (nAChR), with a Ki value of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively, in the striatum of rats. |
|
|
S4143 |
Pentoxyverine Citrate
|
Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. |
|
|
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. |
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S6518 |
Desmethylanethol trithione
|
Desmethylanethol trithione (ADT-OH) is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor. |
|
|
E3116 |
Acanthopanax Senticosus Extract
|
Acanthopanax Senticosus Extract is obtained from Acanthopanax Senticosus, which exhibits dual effects of contraction via muscarinic ACh receptors (mAChRs) and direct relaxation on mouse ileal function, and its relaxant effect could be useful in treating diarrhea symptoms, resulting in an increase in the parasympathetic nerve activities. |
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S4619 |
Itopride hydrochloride
|
Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM. |
|
|
E1876New |
GTS-21 dihydrochloride
|
GTS-21 dihydrochloride(DMXB-A, DMBX-anabaseine) is a selective agonist of alpha7 nicotinic acetylcholine receptor (α7-nAChR) and exhibits anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also an antagonist of α4β2 with a Ki value of 20 nM for humanα4β2 and 5-HT3A receptor with an IC50 value of 3.1 μM. |
|
|
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. |
|
|
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. |
|
|
S7366 |
LY2119620
|
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
|
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S9459 |
Mecamylamine Hydrochloride
|
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR(nicotinic acetylcholine receptors) antagonist.It is also a ganglionic blocker and can across the blood-brain barrier. It can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area. |
|
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E3612 |
Cremastra appendiculata Extract
|
Cremastra Appendiculata Extract is extracted from Cremastra appendiculata (Pseudobulbus Cremastrae seu Pleiones), the dried pseudostem of plants of the Orchidaceae family. Cremastra appendiculata has antibacterial, antihypertensive, gout, antitumor, and acetylcholine receptor M3-blocking effects. The extract of cremastra appendiculata can be used to treat Lewis lung cancer, liver cancer, and breast cancer. |
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E0829 |
Nitrocaramiphen hydrochloride
|
Nitrocaramiphen hydrochloride is an antagonist of muscarinic acetylcholine receptor M1 (mAChR M1), which can completely remove the hyperpolarizing effect of muscarine. |
|
|
E2874 |
Sofpironium bromide
|
Sofpironium bromide (BBI 4000) is an anticholinergic agent that reduces sweat by inhibiting M3 muscarinic receptors in eccrine glands. |
|
|
E0755 |
Guvacoline hydrochloride
|
Norarecoline hydrochloride (Guvacoline hydrochloride) is a pyridine alkaloid found in Areca triandra, which can act as a full agonist at both atrial and ileal muscarinic receptors. |
|
|
E4714New |
Xanomeline
|
Xanomeline(LY-246708) is a selective agonist of muscarinic type 1(M(1) receptor and muscarinic type 4 receptor(M(4). It increases neuronal excitability and inhibits behaviors induced by D-amphetamine and (-)-apomorphine. |
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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.
|
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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. |
|
|
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. |
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E3223 |
Alpiniae Officinarum Rhizoma Extract
|
Alpiniae Officinarum Rhizoma Extract is extracted from Alpiniae Officinarum Rhizoma, which inhibits acetylcholinesterase (AChE) and can be used for the treatment of Alzheimer's disease. |
|
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S4623 |
Methylbenactyzine Bromide
|
Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity. |
|
|
E0799 |
VU 0365114
|
VU 0365114 is a muscarinic acetylcholine receptor M5-preferring (mAChR M5-preferring) positive allosteric modulator (PAM) with an EC50 of 2.7 μM. |
|
|
E4298 |
(-)-Carvone
|
(-)-Carvone is an insect neurotoxin and is an irreversible inhibitor of acetylcholinesterase (AChE). It can be used as a bird repellent, inhibits larval growth, decreases pupation rate, and increases the mortality of larvae. |
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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. |
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S4069 |
Hexamethonium Dibromide
|
Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia. |
|
|
S4072 |
Decamethonium Bromide
|
Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent. |
|
|
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. |
|
|
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. |
|
|
E1265 |
Deschloroclozapine
|
Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs (muscarinic Designer Receptors Exclusively Activated by Designer Drugs) agonist, and binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. |
|
|
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. |
|
|
S3769 |
Palmatine
|
Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities. |
-
Eur J Pharmacol, 2024, 967:176395
|
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E0382 |
W-84 Dibromide
|
W-84 dibromide (HDMPPA) is a potent allosteric modulator of M2-acetylcholine receptors, which retards 3HN-methylscopolamine dissociation. |
|
|
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. |
|
|
S5850 |
Vasicine
|
Vasicine, an alkaloid isolated from A. vasica, is a potential natural cholinesterase inhibitor, exhibits promising anticholinesterase activity in preclinical models and has been in development for treatment of Alzheimer’s disease. |
|
|
S3788 |
Carvacrol
|
Carvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities. |
|
|
S9087 |
Tenuifolin
|
Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
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. |
|
|
S5931 |
BQCA
|
BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR). |
|
|
S3735 |
Umeclidinium bromide
|
Umeclidinium bromide(GSK573719A) is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). |
|
|
S5538 |
Tropisetron
|
Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
-
Chin Med, 2024, 19(1):87
-
Neural Regen Res, 2023, 18(9):2019-2028
|
|
S5075 |
Acotiamide
|
Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties. |
|
|
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. |
|
|
S2957 |
Encenicline (EVP-6124) hydrochloride
|
Encenicline (EVP-6124) hydrochloride is a selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. |
|
|
E0176 |
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.
|
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|
E0831 |
Pseudocoptisine chloride
|
Pseudocoptisine chloride (Isocoptisine chloride) is a quaternary alkaloid with benzylisoquinoline skeleton isolated from Corydalis Tuber, inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM, showing anti-inflammatory and anti-amnestic effects. |
|
|
E2237 |
Vasicine (hydrochloride)
|
Vasicine hydrochloride(Peganine hydrochloride) is a salt of vasicine (VAS), an alkaloid isolated from Adhatoda vasica, is a potential natural cholinesterase inhibitor. VAS inhibits both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). |
|
|
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. |
|
|
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. |
|
|
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 (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class. |
|
|
S5511 |
Ethyl (triphenylphosphoranylidene) acetate
|
Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
|
|
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. |
|
|
S6469 |
Thonzylamine
|
Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
|
|
S0457 |
DREADD agonist 21
|
DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM. |
|
|
S2082 |
Adiphenine HCl
|
Adiphenine HCl(NSC 129224) is a nicotinic receptor inhibitor, used as an antispasmodic drug. |
|
|
S9475 |
Hupehenine
|
Hupehenine is a steriodal alkaloid extracted from the bulbs of Fritillaria Hupehensis, with the potential for inhibiting acetylcholine, antagonism for muscarinic receptors and cholinesterase inhibition. |
|
|
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. |
|
|
S5100 |
Pralidoxime Iodide
|
Pralidoxime Iodide (2-PAM) is an antidote approved for reactivation of inhibited acetylcholinesterase (AChE) in organophosphate poisoning. |
|
|
S4389 |
Bephenium Hydroxynaphthoate
|
Bephenium(NSC 759245) 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. |
|
|
S5747 |
Morantel tartrate
|
Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs). |
|
|
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. |
|
|
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). |
|
|
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. |
|
|
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. |
|
|
S9179 |
Catharanthine hemitartrate
|
Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
|
|
S4292 |
Diphenidol HCl
|
Diphenidol HCl(Diphenidol hydrochloride) 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.
|
|
|
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. |
|
|
S0702 |
α-Conotoxin GI
|
α-Conotoxin GI, a 13-residue peptide originally isolated from the venom of the fish-hunting cone snail Conus geographus, acts as a competitive antagonist for the muscle-type nicotinic acetylcholine receptor (nAChR) with excellent selectivity for α/δ receptor subunit binding over α/γ. |
|
|
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. |
|
|
S1913 |
Tropicamide
|
Tropicamide(Ro 1-7683) is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM. |
|
|
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. Vinblastine sulfate induces autophagy and apoptosis. |
- Nat Commun, 2023, 14(1):7576
- J Immunother Cancer, 2023, 11(8)e007253
- J Immunother Cancer, 2023, 10.1136/jitc-2023-007253
|
|
S2462 |
Donepezil HCl
|
Donepezil HCl is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration. |
- Theranostics, 2023, 13(6):1826-1842
- J Cell Physiol, 2023, 10.1002/jcp.31057
- Comp Biochem Physiol C Toxicol Pharmacol, 2023, 272:109698
|
|
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. |
- Nat Commun, 2023, 10.1038/s41467-023-42332-0
- Nat Commun, 2023, 14(1):6690
- iScience, 2023, 26(8):107477
|
|
S2452 |
Amfebutamone (Bupropion) HCl
|
Amfebutamone (Bupropion) HCl(Wellbutrin) 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
- G3 (Bethesda), 2014, 10.1534/g3.114.010819
|
|
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. |
- Theranostics, 2023, 13(6):1826-1842
- Front Bioeng Biotechnol, 2022, 10:855755
- Front Cardiovasc Med, 2021, 8:639541
|
|
S3047 |
Otilonium Bromide
|
Otilonium bromide is an antimuscarinic. |
- Biochem Pharmacol, 2023, 215:115746
- Res Microbiol, 2022, S0923-2508(22)00073-0
|
|
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. |
- J Cell Physiol, 2023, 10.1002/jcp.31057
- Mol Psychiatry, 2018, 23(3):767-776
|
|
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
|
|
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. |
- Kaohsiung J Med Sci, 2023, none
- Acta Pharmacol Sin, 2021, 1-11
|
|
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
|
|
S1339 |
Galanthamine HBr
|
Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. |
- J Cell Physiol, 2023, 10.1002/jcp.31057
|
|
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
|
|
S4014 |
Hyoscyamine
|
Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM. |
- Theranostics, 2022, 12(12):5488-5503
|
|
S5900 |
Edrophonium chloride
|
Edrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase. |
- Int J Mol Sci, 2023, 10.3390/ijms242115535
|
|
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
|
|
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
|
|
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. |
|
|
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
|
|
S2378 |
Butylscopolamine Bromide
|
Butylscopolamine Bromide (Scopolamine Butylbromide,(-)-Scopolamine butylbromide, Hyoscine butylbromide), is a peripherally acting antimuscarinic, anticholinergic agent used as an abdominal-specific antispasmodic. |
|
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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. |
|
|
S1397 |
Rocuronium Bromide
|
Rocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia. |
|
|
S1929 |
Irsogladine
|
Irsogladine(Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
|
|
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. |
|
|
E3551 |
Stephania Extract
|
Stephania Extract is extracted from Stephania, which ameliorates Scopolamine-Induced Memory Impairment in Mice through Inhibition of Acetylcholinesterase and Oxidative Stress. |
|
|
S9219 |
Huperzine B
|
Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
|
|
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. |
|
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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. |
|
|
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). |
|
|
E4822New |
Tacrine
|
Tacrine is a potent acetylcholinesterase (AChE) inhibitor. It inhibits acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) with an IC50 of 77 nM and 69 nM, respectively. It is used in the treatment of Alzheimer's disease (AD), also poisoning topoisomerases and inhibiting in vivo (mitochondrial)mtDNA synthesis. |
|
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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. |
|
|
E3651 |
Lycopodiastrum casuarinoides Extract
|
Lycopodiastrum casuarinoides Extract is extracted from Lycopodiastrum casuarinoides, which has acetylcholinesterase inhibitory activity. |
|
|
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 (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg. |
|
|
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). |
|
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S9260 |
Nodakenin
|
Nodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM. |
|
|
S3835 |
Loganin
|
Loganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively. |
|
|
S4619 |
Itopride hydrochloride
|
Itopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM. |
|
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E3612 |
Cremastra appendiculata Extract
|
Cremastra Appendiculata Extract is extracted from Cremastra appendiculata (Pseudobulbus Cremastrae seu Pleiones), the dried pseudostem of plants of the Orchidaceae family. Cremastra appendiculata has antibacterial, antihypertensive, gout, antitumor, and acetylcholine receptor M3-blocking effects. The extract of cremastra appendiculata can be used to treat Lewis lung cancer, liver cancer, and breast cancer. |
|
|
E2874 |
Sofpironium bromide
|
Sofpironium bromide (BBI 4000) is an anticholinergic agent that reduces sweat by inhibiting M3 muscarinic receptors in eccrine glands. |
|
|
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. |
|
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E3223 |
Alpiniae Officinarum Rhizoma Extract
|
Alpiniae Officinarum Rhizoma Extract is extracted from Alpiniae Officinarum Rhizoma, which inhibits acetylcholinesterase (AChE) and can be used for the treatment of Alzheimer's disease. |
|
|
E4298 |
(-)-Carvone
|
(-)-Carvone is an insect neurotoxin and is an irreversible inhibitor of acetylcholinesterase (AChE). It can be used as a bird repellent, inhibits larval growth, decreases pupation rate, and increases the mortality of larvae. |
|
|
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. |
|
|
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. |
|
|
S3769 |
Palmatine
|
Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities. |
- Eur J Pharmacol, 2024, 967:176395
|
|
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. |
|
|
S5850 |
Vasicine
|
Vasicine, an alkaloid isolated from A. vasica, is a potential natural cholinesterase inhibitor, exhibits promising anticholinesterase activity in preclinical models and has been in development for treatment of Alzheimer’s disease. |
|
|
S3788 |
Carvacrol
|
Carvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities. |
|
|
S9087 |
Tenuifolin
|
Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
|
|
S3884 |
Jatrorrhizine
|
Jatrorrhizine (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. |
|
|
S5075 |
Acotiamide
|
Acotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties. |
|
|
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. |
|
|
E0831 |
Pseudocoptisine chloride
|
Pseudocoptisine chloride (Isocoptisine chloride) is a quaternary alkaloid with benzylisoquinoline skeleton isolated from Corydalis Tuber, inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM, showing anti-inflammatory and anti-amnestic effects. |
|
|
E2237 |
Vasicine (hydrochloride)
|
Vasicine hydrochloride(Peganine hydrochloride) is a salt of vasicine (VAS), an alkaloid isolated from Adhatoda vasica, is a potential natural cholinesterase inhibitor. VAS inhibits both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). |
|
|
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 (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class. |
|
|
S5511 |
Ethyl (triphenylphosphoranylidene) acetate
|
Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
|
|
S2082 |
Adiphenine HCl
|
Adiphenine HCl(NSC 129224) is a nicotinic receptor inhibitor, used as an antispasmodic drug. |
|
|
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. |
|
|
S9560 |
Anisodamine Hydrobromide
|
Anisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs). |
|
|
S4838 |
Acotiamide hydrochloride
|
Acotiamide Hydrochloride (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. |
|
|
S9179 |
Catharanthine hemitartrate
|
Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
|
|
S2497 |
Pancuronium dibromide
|
Pancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant. |
- bioRxiv, 2024, 2024.05.23.595327
- Biomedicines, 2022, 10(12)3056
- Elife, 2019, 8e45399
|
|
S2508 |
Scopolamine (LSM-4015) HBr
|
Scopolamine HBr (LSM-4015,NSC 61806,(-)-Scopolamine hydrobromide, Hyoscine hydrobromide, Scopine hydrobromide) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
- Heliyon, 2024, 10(1):e23945
- Zool Res, 2023, 44(4):712-724
- Zool Res, 2023, 44(4):712-724
|
|
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
|
|
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
|
|
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. |
- Neurosci Bull, 2023, none
- Neurochem Res, 2020, 10.1007/s11064-020-03103-1
|
|
S3144 |
Darifenacin HBr
|
Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. |
- AAPS PharmSciTech, 2024, 25(7):204
- World J Gastroenterol, 2023, 29(20):3103-3118
- JCI Insight, 2017, 2(3):e89780
|
|
S2549 |
Trospium chloride
|
Trospium chloride is a competitive muscarinic cholinergic receptor antagonist. |
- FEBS Lett, 2020, 10.1002/1873-3468.14015
|
|
S4713 |
Atropine
|
Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
- iScience, 2023, 26(3):106241
|
|
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
|
|
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. |
- J Clin Med, 2022, 11(9)2307
|
|
S3117 |
Oxybutynin hydrochloride
|
Oxybutynin(MJ4309-1) is an anticholinergic medication used to relieve urinary and bladder difficulties. |
- Environ Toxicol Chem, 2021, 10.1002/etc.5018
|
|
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. |
|
|
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 (YM905) is a urinary antispasmodic of the antimuscarinic class. |
|
|
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. |
|
|
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. |
|
|
S5480 |
Clidinium Bromide
|
Clidinium Bromide(Ro 2-3773) is an anticholinergic drug. |
|
|
S6985 |
Varenicline
|
Varenicline(CP 526555) 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. |
|
|
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. |
|
|
S9326 |
Scopolamine
|
Scopolamine (Skopolamin) is a tropane alkaloid derived from plants of the nightshade family, specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties. |
- Immunity, 2024, 57(2):364-378.e9
|
|
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. |
|
|
S2054 |
Orphenadrine Citrate
|
Orphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects. |
|
|
S4034 |
Diphemanil Methylsulfate
|
Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR). |
|
|
S4143 |
Pentoxyverine Citrate
|
Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. |
|
|
E3116 |
Acanthopanax Senticosus Extract
|
Acanthopanax Senticosus Extract is obtained from Acanthopanax Senticosus, which exhibits dual effects of contraction via muscarinic ACh receptors (mAChRs) and direct relaxation on mouse ileal function, and its relaxant effect could be useful in treating diarrhea symptoms, resulting in an increase in the parasympathetic nerve activities. |
|
|
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. |
|
|
S9459 |
Mecamylamine Hydrochloride
|
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR(nicotinic acetylcholine receptors) antagonist.It is also a ganglionic blocker and can across the blood-brain barrier. It can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area. |
|
|
E0829 |
Nitrocaramiphen hydrochloride
|
Nitrocaramiphen hydrochloride is an antagonist of muscarinic acetylcholine receptor M1 (mAChR M1), which can completely remove the hyperpolarizing effect of muscarine. |
|
|
S3701 |
Benactyzine hydrochloride
|
Benactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety.
|
|
|
S5699 |
Scopolamine N-Oxide HydrobroMide Monohydrate
|
Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. |
|
|
S4623 |
Methylbenactyzine Bromide
|
Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity. |
|
|
S4069 |
Hexamethonium Dibromide
|
Hexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia. |
|
|
S3735 |
Umeclidinium bromide
|
Umeclidinium bromide(GSK573719A) is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). |
|
|
S5538 |
Tropisetron
|
Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
- Chin Med, 2024, 19(1):87
- Neural Regen Res, 2023, 18(9):2019-2028
|
|
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. |
|
|
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. |
|
|
S6469 |
Thonzylamine
|
Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
|
|
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. |
|
|
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(Diphenidol hydrochloride) 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.
|
|
|
S0702 |
α-Conotoxin GI
|
α-Conotoxin GI, a 13-residue peptide originally isolated from the venom of the fish-hunting cone snail Conus geographus, acts as a competitive antagonist for the muscle-type nicotinic acetylcholine receptor (nAChR) with excellent selectivity for α/δ receptor subunit binding over α/γ. |
|
|
S1913 |
Tropicamide
|
Tropicamide(Ro 1-7683) is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM. |
|
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