AChR

AChR抑制剂选择性比较

AChR信号通路图

AChR信号通路图

AChR产品

  • 所有产品(156)
  • AChR抑制剂 (60)
  • AChR激活剂 (3)
  • AChR拮抗剂 (45)
  • AChR激动剂 (31)
  • AChR调节剂 (13)
目录号 产品名 产品描述 文献引用 实验数据
S2462 Donepezil HCl Donepezil HCl 是一种特异性的,有效的AChE抑制剂,作用于bAChEhAChEIC50分别为8.12 nM和11.6 nM。
Front Bioeng Biotechnol, 2022, 10:855755
Analyst, 2022, 10.1039/d2an00031h
Front Cardiovasc Med, 2021, 8:639541
S2251 (-)-Huperzine A (HupA) (-)-Huperzine A (HupA)是一种有效的,高度特异性的,可逆acetylcholinesterase (AChE)(乙酰胆碱酯酶)抑制剂,Ki为7 nM,作用于G4 AChE比作用于G1 AChE选择性高200倍。Phase 4。
Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
E0831New Pseudocoptisine chloride Pseudocoptisine chloride (Isocoptisine chloride)是一种分离自Corydalis Tuber具有苄基异喹啉骨架的季生物碱,抑制乙酰胆碱酯酶(acetylcholinesterase, AChE)活性,IC50为12.8 μM,具有抗炎和抗健忘的作用。
S2452 Amfebutamone (Bupropion) HCl Amfebutamone (Bupropion) HCl是一种选择性去甲肾上腺素-多巴胺再摄取的抑制剂,IC50分别为6.5和3.4μM。
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
Georgia State University, 2014, Chaquettea Felton
S1339 Galanthamine HBr Galanthamine HBr是一种AChE抑制剂,IC50为0.35 μM,比作用于丁酰胆碱酯酶选择性高50倍。
S4031 Aclidinium Bromide Aclidinium Bromide (LAS 34273, LAS-W 330)与人源毒蕈碱受体AChR M1, M2, M3, M4和M5结合,Ki值分别为0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM和0.16 nM。
S1397 Rocuronium Bromide Rocuronium Bromide (ORG 9426) 是一种氨基甾体类非去极化的神经肌肉受体抑制剂或肌肉松弛剂。
S3047 Otilonium Bromide Otilonium Bromide是一种抗毒蕈碱药物.
S2471 Gallamine Triethiodide Gallamine Triethiodide 是一种胆碱能受体抑制剂,IC50为68.0±8.4 μM。
Mol Cell, 2019, 75(1):53-65
S1608 Pyridostigmine Bromide Pyridostigmine Bromide 是一种拟副交感神经的和可逆的胆碱酯酶抑制剂。
J Am Heart Assoc, 2014, 3(3):e000804
S2087 Rivastigmine Tartrate Rivastigmine Tartrate (ENA 713) 是一种胆碱酯酶抑制剂,IC50为5.5 μM,作为副交感神经或胆碱能剂,用于治疗轻度至中度阿尔茨海默病。
Mol Psychiatry, 2018, 23(3):767-776
S1929 Irsogladine Irsogladine是一种抗胃溃疡剂,通过M1 muscarininc乙酰胆碱受体结合,有利于细胞间隙连接通讯。
S2490 Neostigmine Bromide Neostigmine Bromide 是一种可逆的胆碱酯酶抑制剂。
Am J Physiol Gastrointest Liver Physiol, 2016, 310(3):G181-92
S3202 Catharanthine Catharanthine是一种从长春花中分离出来的生物碱,可以抑制烟碱受体介导的隔膜收缩,IC50为59.6µM。
S5073 Donepezil Donepezil (Aricept, Donepezilo)是一种有效的、可逆的、特异的和非竞争性acetylcholinesterase (AChE)抑制剂,用于治疗轻度至中度痴呆。
Front Bioeng Biotechnol, 2022, 10:855755
Front Cardiovasc Med, 2021, 8:639541
Int J Pharm, 2019, 560:294-305
S3245 Nodakenetin Nodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素,可抑制 α-glucosidasePTP1Brat lens aldose reductase (RLAR)AChEBChEβ-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 BaxBcl-2 的蛋白质表达,并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。
S4014 Hyoscyamine Hyoscyamine (Daturine) 是一种AChR抑制剂,IC50为7.5nM。
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) 是acetylcholinesterase (AChE)的可逆性抑制剂,不能穿透血脑屏障,用于治疗重症肌无力。
S3246 Picfeltarraenin IB Picfeltarraenin IB 是从 Picriafel-terrae 中分离出的葫芦素糖苷,是 acetylcholinesterase (AChE) 的抑制剂。Picfeltarraenin IB 可用于治疗疱疹感染,癌症和炎症。
S5385 Imidafenacin Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3).
S4023 Procaine HCl Procaine (Novocaine) 是一种钠离子通道的,NMDA受体以及乙酰胆碱受体抑制剂, IC50分别为60 μM, 0.296 mM何45.5 μM,也是一种,5-HT3抑制剂,KD为1.7 μM。
Biomol Ther (Seoul), 2016, 24(5):489-94
Biomol Ther (Seoul), 2016, 24(5):489-94
S3820 Dehydroevodiamine hydrochloride Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production.
S5900 Edrophonium chloride Edrophonium chloride是edrophonium的氯盐形式。Edrophonium是一种快速起效、短效、易可逆的acetylcholinesterase (乙酰胆碱酯酶)抑制剂。
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)是一种神经肌肉抑制剂,ED95为0.2 mg/kg。
S0766 RHC 80267 RHC 80267 (U-57908) 是一种有效的、具有选择性的 diacylglycerol lipase (DAGL, DAG lipase) 的抑制剂,其对 cholinesterase 活性的IC50值为4 μM。RHC 80267 可抑制 cyclooxygenase (COX) 的活性,phospholipase C (PLC) 的活性和 phosphatidylcholine (PC) 的水解作用。
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 是一种有效的 nicotine acetylcholine receptor (nAChR) 的选择性抑制剂,其对 α6β2 nAChRα4β2 nAChR 的Ki值分别为0.12 nM 和0.14 nM。
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) 是一种AChE抑制剂。其IC50为2.04 +/- 0.27 μM。
S4162 Benzethonium Chloride Benzethonium chloride 是有效的neuronal nicotinic acetylcholine receptors (nAChRs)(神经元烟碱型乙酰胆碱受体)抑制剂,抑制α4β2 nAChRsα7 nAChRsIC50分别为49 nM 和 122 nM。
Front Cell Infect Microbiol, 2021, 11:630812
Am J Cancer Res, 2019, 9(11):2397-2412
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate 是一种抗组胺药、抗焦虑药和抗血清素的化合物,是多种monoamine receptors,包括多种 serotonin receptors 的高效拮抗剂。Pimethixene maleate 可抑制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 和 Muscarinic M2,对应的pKi值分别为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和9.38。
S3639 Tacrine hydrochloride hydrate Tacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) 是胆碱酯酶(cholinesterase)抑制剂,可对抗骨骼肌松弛药的作用,可作为呼吸兴奋剂并用于治疗阿兹海默病和其他中枢神经系统障碍。它也是组胺N-甲基转移酶(histamine N-methyltransferase)抑制剂。
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 是次要的烟草生物碱之一,并存在于各种食品中。Myosmine 对 a4b2 nicotinic acetylcholinergic receptors (nAChR) 具有低亲和力,Ki为3300 nM。
S3769 Palmatine Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.
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.
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.
S4505 Vinblastine (NSC-49842) sulfate Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe)抑制微管形成nAChR活性,在无细胞实验的测定中,IC50为8.9 μM。Vinblastine sulfate 可诱导自噬和凋亡。
J Pharm Biomed Anal, 2022, 215:114772
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
S5075 Acotiamide Acotiamide (Acofide, Z388)是一种新型的乙酰胆碱酯酶(AChE)抑制剂,具有促胃动力和眼底松弛的效果。
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.
S4687 Rivastigmine Rivastigmine (SDZ-ENA 713, Exelon) 是一种胆碱酯酶的抑制剂,IC50为5.5 μM。它抑制乙酰胆碱酯酶(IC50=4.15 µM)和丁酰胆碱酯酶(IC50=37 nM)。
Nature, 2018, 560(7718):372-376
S4776 Harmaline Harmaline, a natural occurrence β-carboline alkaloid, is a central nervous system stimulant and an acetylcholinesterase (AChR) inhibitor; also inhibits histamine N-methyltransferase.
S3903 Lycorine Lycorine (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.
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)是一种抗毒蕈碱类的抗帕金森病药物。
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 是一种烟碱受体抑制剂,用作解痉药。
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.
S0016 SN-6 SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3,对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。
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.
Neurotherapeutics, 2021, 10.1007/s13311-021-01052-3
S9560 Anisodamine Hydrobromide Anisodamine (6-Hydroxyhyoscyamine)是天然存在的阿托品(atropine)衍生物,具有消炎活性。它能抑制α1-adrenergic receptorsmAChRs
S4838 Acotiamide hydrochloride Acotiamide Hydrochloride (YM-443, Z-338)是acotiamide的盐酸形式,acotiamide是一种肠蠕动促进剂。它是一种新型的、具有口服活性的、选择性的AChE抑制剂。
S9179 Catharanthine hemitartrate Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine.
S5493 Atropine sulfate Atropine Sulfate (Sulfatropinol, Atropette, Tropintran) is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects.
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S4575 Pralidoxime chloride Pralidoxime chloride (2-PAM)是有机磷农药和一些化学制品的解毒剂。是AChE的重新激活剂。
S5100 Pralidoxime Iodide Pralidoxime Iodide (2-PAM)是一种解毒剂,有机磷中毒后可重新激活被抑制的AChE。
S4389 Bephenium Hydroxynaphthoate Bephenium 是一种 B-type Acetylcholine receptor (AChR) 的激活剂。Bephenium 可选择性地激活由Hco-UNC-29.1,Hco-UNC-38,Hco-UNC-63,Hco-ACR-8亚基组成的Hco-L-AChR1亚型。Bephenium hydroxynaphthoate 是一种驱虫药,以前用于治疗钩虫感染和蛔虫病。
S2547 Tiotropium Bromide hydrate Tiotropium Bromide hydrate (BA 679BR)是Tiotropium bromide (Spiriva; Tiova; BA 679BR; Tiopropium)的一水合物,是抗胆碱药,支气管扩张剂及毒蕈碱受体拮抗剂。
S2497 Pancuronium dibromide Pancuronium dibromide是一种竞争性的乙酰胆碱受体拮抗剂,用作肌肉松弛剂。
Elife, 2019, 8e45399
Front Physiol, 2019, 10:1039
Scholars' Bank, 2019, N/A
E0829New Nitrocaramiphen hydrochloride Nitrocaramiphen hydrochloride是毒蕈碱乙酰胆碱受体 M1 (muscarinic acetylcholine receptor M1, mAChR M1)的拮抗剂,可完全消除毒蕈碱的超极化作用。
S2550 Tolterodine tartrate Tolterodine tartrate (PNU-200583E)是Tolterodine的酒石酸盐形式,是一种竞争性的毒蕈碱型乙酰胆碱受体拮抗剂。
JCI Insight, 2019, 4(20)
S2240 Fesoterodine Fumarate Fesoterodine Fumarate (SPM 907) 是毒蕈碱受体拮抗剂5-羟甲基托特罗定的前药,用来治疗膀胱过度活动症。
Hum Mol Genet, 2020, ddaa244
S1754 Oxybutynin Oxybutynin 是一种竞争性的muscarinic acetylcholine receptorM1,M2,和M3拮抗剂,用于减少尿量,减轻膀胱负担。
S3048 Solifenacin succinate Solifenacin succinate (YM905)是一种抗毒蕈碱类泌尿解痉药。
S1683 Ipratropium Bromide Ipratropium bromide是毒蕈碱拮抗剂,支气管扩张剂,是AtropineN的异丙基盐。
Int Forum Allergy Rhinol, 2020, 10(2):233-242
Anal Chem, 2019, 91(18):11888-11896
S2549 Trospium chloride Trospium chloride 是一种竞争性的毒蕈碱型乙酰胆碱受体拮抗剂。
FEBS Lett, 2020, 10.1002/1873-3468.14015
S2130 Atropine sulfate monohydrate Atropine sulfate monohydrate是一种竞争性毒蕈碱型乙酰胆碱受体拮抗剂,IC50为2.5 nM。
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S1978 Methscopolamine Methscopolamine是一种毒蕈碱型乙酰胆碱受体抑制剂。
Mol Brain, 2021, 14(1):113
Mol Neurobiol, 2020, 10.1007/s12035-020-02175-y
Neuropharmacology, 2019, 146:252-263
S2508 Scopolamine (LSM-4015) HBr Scopolamine HBr (LSM-4015, NSC 61806)是一种竞争性的毒蕈碱型乙酰胆碱受体拮抗剂,IC50为55.3 ± 4.3 nM。
Exp Ther Med, 2020, 20(4):3625-3632
Mol Cell, 2019, 75(1):53-65
Autophagy, 2019, 10.1080/15548627.2019.1630224
S2659 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)是一种新的蕈毒碱受体拮抗剂,Kb为0.84 nM.
S3144 Darifenacin HBr Darifenacin HBr (UK-88525)是一种选择性的M3 muscarinic(M3蕈毒碱)受体拮抗剂,pKi为8.9。
JCI Insight, 2017, 2(3):e89780
S5873 Scopolamine HBr trihydrate Scopolamine HBr是一种竞争性的蕈毒碱型乙酰胆碱受体(muscarinic acetylcholine receptor)拮抗剂,IC50为55.3 nM。
S4931 Propiverine hydrochloride Propiverine是一种抗胆碱能药物,用于治疗膀胱过度活动症和尿失禁。
S0032 Batefenterol  Batefenterol (GSK961081, TD-5959) 既是 muscarinic receptor 的拮抗剂又是 β2-adrenoceptor 的激动剂,hM2、hM3 muscarinic receptors 和 hβ2-adrenoceptor 的Ki值分别为1.4 nM、1.3 nM和3.7 nM。
S4713 Atropine Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) 是一种具有竞争性的 muscarinic acetylcholine receptor (mAChR) 的拮抗剂,具有抗近视作用。
S5480 Clidinium Bromide Clidinium Bromide is an anticholinergic drug.
S4024 Homatropine Methylbromide Homatropine Methylbromide是一种毒蕈碱受体AChR拮抗剂,抑制WKY-E和SHR-E , IC50分别为162.5 nM和170.3 nM。
Nature, 2018, 560(7718):372-376
S6985 Varenicline Varenicline具有高度选择性,对α4β2 receptors的阻断作用比其他烟碱受体高500倍以上,比非烟碱受体和转运蛋白高2000倍以上。Varenicline 还可作为5-HT3 serotonine receptors的激动剂。
S4025 Homatropine Bromide Homatropine Bromide是一种毒蕈碱受体AChR拮抗剂,抑制WKY-E和SHR-E , IC50分别为162.5 nM和170.3 nM。
S4027 Flavoxate HCl Flavoxate (NSC-114649)是一种毒蕈碱受体AChR拮抗剂, IC50为12.2 μM.
S5238 Solifenacin (YM905) Solifenacin (YM905) is a competitive muscarinic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle.
S5258 Revefenacin Revefenacin (TD-4208, 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 是一种骨骼肌松弛剂,作用于中枢神经系统,产生肌肉松弛作用。
S4034 Diphemanil Methylsulfate Diphemanil Methylsulfate是一种季铵抗胆碱能药剂,可以结合毒蕈碱型乙酰胆碱受体(mAchR)。
S4143 Pentoxyverine Citrate Pentoxyverine Citrate (Carbetapentane) 是antitussive(止咳药),通常用于治疗咳嗽相关的疾病,如感冒。
S5777 Ipratropium bromide monohydrate Ipratropium bromide (Atrovent, Sch 1000) monohydrate 是 muscarinic acetylcholine receptors (mAChR) 的拮抗剂,对M1、M2和M3受体的IC50值分别为2.9 nM、2.0 nM和1.7 nM。
S3701 Benactyzine hydrochloride Benactyzine hydrochloride是中枢性毒蕈碱受体拮抗剂。在抑郁症和相关焦虑的治疗中,它被用作抗抑郁剂。
S5699 Scopolamine N-Oxide HydrobroMide Monohydrate Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine)是毒蕈碱拮抗剂,用于研究m型胆碱能受体的结合特性。
S4623 Methylbenactyzine Bromide Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) 是一种毒蕈硷胆碱能受体拮抗剂,具有解痉活性。
S4069 Hexamethonium Dibromide Hexamethonium Dibromide是一种神经中枢中选择性的神经元烟碱型AChR选择性拮抗剂。
S4660 Glycopyrrolate Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn)是毒蕈碱拮抗剂。在胃肠道疾病中,被用作止痉挛药。
J Clin Med, 2022, 11(9)2307
S3735 Umeclidinium bromide Umeclidinium bromide是一种长效毒蕈碱拮抗剂,对治疗慢性阻塞性肺疾病具有持续性疗效。
S5538 Tropisetron Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
S3117 Oxybutynin hydrochloride Oxybutynin chloride是一种抗胆碱药,用于缓解尿和膀胱负担。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S4834 Propantheline bromide Propantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan)是一种毒蕈碱拮抗剂,用于治疗和肠痉挛相关的胃肠道疾病、在麻醉过程中减少分泌。
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) 是抗组胺剂和抗胆碱能药。
S3298 Caulophylline (N-Methylcytisine) Caulophylline (N-Methylcytisine, Caulophyllin, NMC) 是一种具有抗炎活性的三环喹喔啉生物碱。Caulophylline 可与鱿鱼视神经节的 nicotinic acetylcholine receptors (nAChR) 结合,Kd值为50 nM。Caulophylline 可显著地降低 myeloperoxidase (MPO) 的活性,并通过抑制 IκBIKK 磷酸化来阻断 NF-κB 的活化。
S5921 Cyclopentolate Hydrochloride Cyclopentolate是毒蝇碱型乙酰胆碱受体拮抗剂,对M1、M2和M3受体的Ki值分别为1.62, 27.5和2.63 nM。
S4292 Diphenidol HCl Diphenidol HCl是一种有效的muscarinic M2 and M3 receptor拮抗剂,pKb分别为6.72和7.02,用于呕吐和晕眩的治疗。
S0702 α-Conotoxin GI α-ConotoxinGI最初是从鸡心螺的猎鱼毒液中分离出来的13残基肽,作为肌肉型烟碱型乙酰胆碱受体(Nicotinic acetylcholine receptors, nAChRs)的竞争性拮抗剂,相对α/γ来说,对α/δ受体亚单位结合具有极好的选择性。
S1913 Tropicamide Tropicamide是一种抗胆碱,毒蕈碱受体M4亚型的选择性拮抗剂,IC50为8.0 nM。
S1356 Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) 是一种抗癫痫化合物。Levetiracetam (UCB-L059, SIB-S1) 是 muscarinic acetylcholine receptors (mAChR) 的激动剂并能调节突触前P/Q型压敏钙离子通道 calcium (Ca2+) channel
Anticancer Res, 2021, 41(2):687-697
PLoS One, 2019, 14(2):e0211644
Sci Rep, 2016, 6:25705
E1265New Deschloroclozapine Deschloroclozapine,Clozapine的一种代谢物,是一种高效的毒蕈碱型设计药物激活专门受体(muscarinic Designer Receptors Exclusively Activated by Designer Drugs, muscarinic DREADD)激动剂,与DREADD的受体亚型hM3Dq和hM4Di结合,Ki分别为6.3和4.2 nM。
E0755New Guvacoline hydrochloride Norarecoline hydrochloride (Guvacoline hydrochloride)是一种在槟榔(Areca triandra)中发现的吡啶类生物碱,可作为心房和回肠毒蕈碱受体的完全激动剂。
E0176New Dinotefuran Dinotefuran (MTI-446) 作为一种新烟碱类化合物,是一种有效的 nAChRs 激动剂,EC50 为 7.8 μM,对 Da2b2 杂合 nAChRs 显示出高杀虫活性。
E0172New Imidacloprid Imidacloprid是一种烟碱型乙酰胆碱受体 (nAChR) 激动剂,具有强效杀虫活性。
S1440 Varenicline Tartrate (CP 526555-18) Varenicline Tartrate (CP 526555-18, Chantix, Champix)是一种烟碱类AChR激动剂,用于治疗吸烟成瘾。
S2455 Bethanechol chloride Bethanechol chloride是一种选择性毒蕈碱受体激动剂,对烟碱受体没有任何效果。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
Exp Physiol, 2020, 10.1113/EP088900
Lung, 2018, 196(2):219-229
S2614 Arecoline HBr Arecoline是一种毒蕈碱型乙酰胆碱受体激动剂。
Oncogene, 2020, 39(11):2437-2449
BMC Mol Cell Biol, 2020, 21(1):80
Oncol Rep, 2015, 33(6):2753-60
S4231 Pilocarpine HCl Pilocarpine HCl (NSC 5746)是非选择性毒蕈碱型乙酰胆碱受体激动剂,用于产生癫痫的实验模型。
Theranostics, 2021, 11(12):5986-6005
Mol Brain, 2021, 14(1):113
Anticancer Res, 2021, 41(2):687-697
S0717 Varenicline (CP 526555) dihydrochloride Varenicline (CP 526555) dihydrochloride 是 α4β2 nicotinic acetylcholine receptor (nAChR)α3β4 nAChR 的有效部分激动剂,EC50分别为2.3 μM和55 μM。Varenicline dihydrochloride 是一种有效的 α7 nAChRs 的完全激动剂,EC50值为18 μM。Varenicline 是可用于戒烟的处方药。
S0720 PNU-282987 PNU-282987 是一种新型的 alpha7 nAChR 选择性激动剂,对大鼠 alpha7 nAChR 的 Ki 为 26 nM。除了 Ki 为 930 nM 的 5-HT3 受体外,PNU-282987 对所有测试的单胺、毒蕈碱、谷氨酸和 GABA 受体均无活性。
S0728 N-Desmethylclozapine N-Desmethylclozapine (Norclozapine, Normethylclozapine), a metabolite of the atypical antipsychotic drug Clozapine, is a potent, allosteric and partial agonist of M1 receptors with EC50 of 115 nM. N-Desmethylclozapine is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation and also a δ-opioid agonist.
S0740 PNU-282987 S enantiomer hydrochloride (S)-PNU-282987 is the absolute stereochemistry form of PNU-282987. PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors (nAChRs) with Ki of 26 nM for the rat receptor. PNU 282987 has negligible activity against α1β1γδ and α3β4 nAChRs as well as a panel of monoamine, muscarinic, glutamate, and GABA receptors, except 5-HT3 with Ki of 930 nM.
S4121 Succinylcholine Chloride Dihydrate Succinylcholine Chloride Dihydrate (Suxamethonium)是一种烟碱AChR激动剂,同时也是一种去极化神经肌肉阻断剂。
S4422 Nitenpyram Nitenpyram是一个nicotinic acetylcholine receptor (AchR)激动剂,用于兽医对家畜和宠物寄生虫的治疗。
Proc Natl Acad Sci U S A, 2020, 117(21):11321-11327
S7366 LY2119620 LY2119620是一种人类M2 and M4 muscarinic acetylcholine receptors的特异变构激动剂。
S2287 Cytisine Cytisine (Baphitoxine, Sophorine)是一种烟碱型乙酰胆碱受体激动剂。
S4171 Choline Chloride Choline chloride是一种季铵盐,作为动物饲料添加剂。它是acetylcholine的前体化合物,在多种代谢过程、脂质代谢中作为甲基供体。
S4072 Decamethonium Bromide Decamethonium Bromide是一种烟碱AChR部分激动剂和神经肌肉阻断剂。
S9789 JHU37152 JHU37152 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq)hM4Di 的Ki值分别为1.8 nM和8.7 nM。在HEK-293细胞中基于荧光和BRET的检测中,对 hM3Dq 和 hM4Di 的EC50值分别为5 nM和0.5 nM。
S9790 JHU37160 JHU37160 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq)hM4Di 的Ki值分别为1.9 nM和3.6 nM。在HEK-293细胞中基于荧光和BRET的检测中,对 hM3Dq 和 hM4Di 的EC50值分别为18.5 nM和0.2 nM。
S6432 Cevimeline Cevimeline (AF 102B, SNI 2011, SNK 508)是一种拟副交感神经药,是毒蕈碱样乙酰胆碱受体M1和M3的激动剂。
S6887 Clozapine N-oxide Clozapine N-oxide (CNO) 是一种 Clozapine (GLXC-06516) 的代谢产物,是 human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs) 的激动剂。Clozapine 是一种有效的 dopamine (DA) 拮抗剂和选择性的 muscarinic M4 receptor 的激动剂。
S3684 Methacholine chloride Methacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors.
S5930 PNU 282987 HCl PNU 282987是一种有效的含α7的神经元烟碱受体(α7-containing neuronal nicotinic acetylcholine receptors)激动剂,对大鼠受体的Ki值为26 nM。
S4359 Carbamoylcholine chloride (Carbachol) Carbamoylcholine chloride (Carbachol, Carbamylcholine chloride, Carbastat, Miostat) 是一种 cholinergic 胆碱能的激动剂,模仿乙酰胆碱对 muscarinic and nicotinic receptors 的作用。
S2957 Encenicline (EVP-6124) hydrochloride Encenicline (EVP-6124) hydrochloride是一种选择性α7烟碱型乙酰胆碱受体(α7 nicotinic acetylcholine receptor, α7 nAChR)部分激动剂,通过增强α7烟碱型乙酰胆碱受体的乙酰胆碱反应来提高记忆力。
S0457 DREADD agonist 21 DREADD agonist 21 是一种有效的 human muscarinic acetylcholine M3 receptors (hM3Dq) 激动剂,其EC50值为1.7 nM。
S1805 Acetylcholine Chloride 化合物Acetylcholine Chloride是一种神经递质,作用于包括人类在内的许多生物的周围神经系统(PNS)和中枢神经系统(CNS)。
Biotechnol Lett, 2020, 42(7):1219-1227
Med Sci Monit, 2019, 25:5389-5400
S4718 Acetylcholine iodide Acetylcholine iodide (Acetylcolina)是一种存在于肌肉神经接点、自主神经节、副交感效应连接处以及中枢神经系统很多地方的神经递质。
Biotechnol Lett, 2020, 42(7):1219-1227
S6795 VU0357017 Hydrochloride VU0357017 hydrochloride (CID-25010775)是一种强效的、中枢神经系统渗透性的高选择性 M1 激动剂,M1是 muscarinic acetylcholine receptors (mAChRs) 的一类亚型。VU0357017 hydrochloride 可在变构位点起作用以激活该受体,其EC50值为 477 nM 和 Ki值为 9.91 μM。
E0799New VU 0365114 VU 0365114 是一种毒蕈碱乙酰胆碱受体M5偏好(muscarinic acetylcholine receptor M5-preferring , mAChR M5-preferring)的正变构调节剂 (positive allosteric modulator, PAM),EC50为2.7 μM。
E0382New W-84 Dibromide W-84 dibromide (HDMPPA)是一种有效的M2-乙酰胆碱受体的变构调节剂,可抑制3HN-甲基多胺的解离。
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) 是一种chloride channel激活剂,用作广谱抗寄生虫药。Ivermectin (MK-933, IVM) 是 P2X4α7 nicotinic acetylcholine receptors (nAChRs) 的特异性正变构效应物。Ivermectin 对 HIV-1 和登革热dengue virus均具有有效的抗病毒活性。Ivermectin 可通过AKT/mTOR信号通路来诱导自噬,并诱导线粒体自噬。
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
S2629 PNU-120596 PNU-120596 (Nsc 216666)是一种有效的α7 nAChR变构调节剂,EC50为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
S0518 NS 1738 NS 1738 (NSC 213859)是一种新型的α7烟碱乙酰胆碱受体(α7 nicotinic acetylcholine receptor, α7 nAChR)正变构调节剂,对非洲蟾卵卵母细胞α7 nAChR具有正向调节作用,EC50为3.4 μM,对大鼠α7 nAChR具有相当的调节作用,EC50为3.9 μM。
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
S0552 BNC210 BNC210 (H-Ile-Trp-OH, IW-2143) 是一种 alpha-7 nicotinic acetylcholine receptor (α7 nAChR) 的负变构调节剂。
S0782 VU0238441 VU0238441 是一种泛 muscarinic acetylcholine receptor (mAChR) 的正向变构调节剂 (PAM),对于M5、M3、M2、M1和M4的EC50值分别为2.1 μM、2.2 μM、2.8 μM、3.2 μM 和 >10 μM。
S0783 VU0119498 VU0119498 是一种泛Gq muscarinic acetylcholine receptor (mAChR) M1,M3,M5的正向变构调节剂(PAM),对应EC50值分别为6.1 μM, 6.4 μM, 4.1 μM。
S5931 BQCA BQCA (benzylquinolone carboxylic acid)是一种高选择性M1 muscarinic acetylcholine receptor (mAChR)正向别构调节剂。
S5844 Lobelin sulphate Lobelin sulphate (Lobeline sulfate, Bantron) 对烟碱性胆碱能受体具有与尼古丁类似的作用。它应用于多种疾病的治疗,如呼吸道疾病、周围性血管疾病、失眠症以及戒烟过程。
S5747 Morantel tartrate Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S2646 VU0238429 VU0238429 (M5 PAM)是第一个 muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) 的阳性变构调节剂,对于M5的EC50值为 1.16 μM,而对于M1和M3的EC50均大于 30 μM。VU0238429 对于M2和M4没有显现出增强剂的活性。
E0524New Spinosad Spinosad是一种具有更广泛作用谱的生物神经毒性杀虫剂,是一种由spinosyns A和D混合而成的,是一种土壤放线菌发酵产物,Spinosad靶向昆虫神经系统的烟碱乙酰胆碱受体 (nicotinic acetylcholine receptor,nAChRs)
S1405 Vecuronium Bromide Vecuronium Bromide (ORG NC45) 是一种肌肉松弛剂,属于非去极化抑制剂。
S4804 1-Naphthyl acetate 1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages.
S4703 Choline bitartrate Choline bitartrate (2-hydroxyethyl(trimethyl)azanium, 2,3,4-trihydroxy-4-oxobutanoate) 是在食物中发现的一种营养性胆碱形式。胆碱对肝、肾脏发挥其正常功能十分重要,是神经递质乙酰胆碱的组成之一。
S2462 Donepezil HCl Donepezil HCl 是一种特异性的,有效的AChE抑制剂,作用于bAChEhAChEIC50分别为8.12 nM和11.6 nM。
Front Bioeng Biotechnol, 2022, 10:855755
Analyst, 2022, 10.1039/d2an00031h
Front Cardiovasc Med, 2021, 8:639541
S2251 (-)-Huperzine A (HupA) (-)-Huperzine A (HupA)是一种有效的,高度特异性的,可逆acetylcholinesterase (AChE)(乙酰胆碱酯酶)抑制剂,Ki为7 nM,作用于G4 AChE比作用于G1 AChE选择性高200倍。Phase 4。
Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
E0831New Pseudocoptisine chloride Pseudocoptisine chloride (Isocoptisine chloride)是一种分离自Corydalis Tuber具有苄基异喹啉骨架的季生物碱,抑制乙酰胆碱酯酶(acetylcholinesterase, AChE)活性,IC50为12.8 μM,具有抗炎和抗健忘的作用。
S2452 Amfebutamone (Bupropion) HCl Amfebutamone (Bupropion) HCl是一种选择性去甲肾上腺素-多巴胺再摄取的抑制剂,IC50分别为6.5和3.4μM。
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
Georgia State University, 2014, Chaquettea Felton
S1339 Galanthamine HBr Galanthamine HBr是一种AChE抑制剂,IC50为0.35 μM,比作用于丁酰胆碱酯酶选择性高50倍。
S4031 Aclidinium Bromide Aclidinium Bromide (LAS 34273, LAS-W 330)与人源毒蕈碱受体AChR M1, M2, M3, M4和M5结合,Ki值分别为0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM和0.16 nM。
S1397 Rocuronium Bromide Rocuronium Bromide (ORG 9426) 是一种氨基甾体类非去极化的神经肌肉受体抑制剂或肌肉松弛剂。
S3047 Otilonium Bromide Otilonium Bromide是一种抗毒蕈碱药物.
S2471 Gallamine Triethiodide Gallamine Triethiodide 是一种胆碱能受体抑制剂,IC50为68.0±8.4 μM。
Mol Cell, 2019, 75(1):53-65
S1608 Pyridostigmine Bromide Pyridostigmine Bromide 是一种拟副交感神经的和可逆的胆碱酯酶抑制剂。
J Am Heart Assoc, 2014, 3(3):e000804
S2087 Rivastigmine Tartrate Rivastigmine Tartrate (ENA 713) 是一种胆碱酯酶抑制剂,IC50为5.5 μM,作为副交感神经或胆碱能剂,用于治疗轻度至中度阿尔茨海默病。
Mol Psychiatry, 2018, 23(3):767-776
S1929 Irsogladine Irsogladine是一种抗胃溃疡剂,通过M1 muscarininc乙酰胆碱受体结合,有利于细胞间隙连接通讯。
S2490 Neostigmine Bromide Neostigmine Bromide 是一种可逆的胆碱酯酶抑制剂。
Am J Physiol Gastrointest Liver Physiol, 2016, 310(3):G181-92
S3202 Catharanthine Catharanthine是一种从长春花中分离出来的生物碱,可以抑制烟碱受体介导的隔膜收缩,IC50为59.6µM。
S5073 Donepezil Donepezil (Aricept, Donepezilo)是一种有效的、可逆的、特异的和非竞争性acetylcholinesterase (AChE)抑制剂,用于治疗轻度至中度痴呆。
Front Bioeng Biotechnol, 2022, 10:855755
Front Cardiovasc Med, 2021, 8:639541
Int J Pharm, 2019, 560:294-305
S3245 Nodakenetin Nodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素,可抑制 α-glucosidasePTP1Brat lens aldose reductase (RLAR)AChEBChEβ-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 BaxBcl-2 的蛋白质表达,并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。
S4014 Hyoscyamine Hyoscyamine (Daturine) 是一种AChR抑制剂,IC50为7.5nM。
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) 是acetylcholinesterase (AChE)的可逆性抑制剂,不能穿透血脑屏障,用于治疗重症肌无力。
S3246 Picfeltarraenin IB Picfeltarraenin IB 是从 Picriafel-terrae 中分离出的葫芦素糖苷,是 acetylcholinesterase (AChE) 的抑制剂。Picfeltarraenin IB 可用于治疗疱疹感染,癌症和炎症。
S5385 Imidafenacin Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3).
S4023 Procaine HCl Procaine (Novocaine) 是一种钠离子通道的,NMDA受体以及乙酰胆碱受体抑制剂, IC50分别为60 μM, 0.296 mM何45.5 μM,也是一种,5-HT3抑制剂,KD为1.7 μM。
Biomol Ther (Seoul), 2016, 24(5):489-94
Biomol Ther (Seoul), 2016, 24(5):489-94
S3820 Dehydroevodiamine hydrochloride Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production.
S5900 Edrophonium chloride Edrophonium chloride是edrophonium的氯盐形式。Edrophonium是一种快速起效、短效、易可逆的acetylcholinesterase (乙酰胆碱酯酶)抑制剂。
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)是一种神经肌肉抑制剂,ED95为0.2 mg/kg。
S0766 RHC 80267 RHC 80267 (U-57908) 是一种有效的、具有选择性的 diacylglycerol lipase (DAGL, DAG lipase) 的抑制剂,其对 cholinesterase 活性的IC50值为4 μM。RHC 80267 可抑制 cyclooxygenase (COX) 的活性,phospholipase C (PLC) 的活性和 phosphatidylcholine (PC) 的水解作用。
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 是一种有效的 nicotine acetylcholine receptor (nAChR) 的选择性抑制剂,其对 α6β2 nAChRα4β2 nAChR 的Ki值分别为0.12 nM 和0.14 nM。
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) 是一种AChE抑制剂。其IC50为2.04 +/- 0.27 μM。
S4162 Benzethonium Chloride Benzethonium chloride 是有效的neuronal nicotinic acetylcholine receptors (nAChRs)(神经元烟碱型乙酰胆碱受体)抑制剂,抑制α4β2 nAChRsα7 nAChRsIC50分别为49 nM 和 122 nM。
Front Cell Infect Microbiol, 2021, 11:630812
Am J Cancer Res, 2019, 9(11):2397-2412
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate 是一种抗组胺药、抗焦虑药和抗血清素的化合物,是多种monoamine receptors,包括多种 serotonin receptors 的高效拮抗剂。Pimethixene maleate 可抑制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 和 Muscarinic M2,对应的pKi值分别为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和9.38。
S3639 Tacrine hydrochloride hydrate Tacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) 是胆碱酯酶(cholinesterase)抑制剂,可对抗骨骼肌松弛药的作用,可作为呼吸兴奋剂并用于治疗阿兹海默病和其他中枢神经系统障碍。它也是组胺N-甲基转移酶(histamine N-methyltransferase)抑制剂。
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 是次要的烟草生物碱之一,并存在于各种食品中。Myosmine 对 a4b2 nicotinic acetylcholinergic receptors (nAChR) 具有低亲和力,Ki为3300 nM。
S3769 Palmatine Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities.
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.
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.
S4505 Vinblastine (NSC-49842) sulfate Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe)抑制微管形成nAChR活性,在无细胞实验的测定中,IC50为8.9 μM。Vinblastine sulfate 可诱导自噬和凋亡。
J Pharm Biomed Anal, 2022, 215:114772
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
S5075 Acotiamide Acotiamide (Acofide, Z388)是一种新型的乙酰胆碱酯酶(AChE)抑制剂,具有促胃动力和眼底松弛的效果。
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.
S4687 Rivastigmine Rivastigmine (SDZ-ENA 713, Exelon) 是一种胆碱酯酶的抑制剂,IC50为5.5 μM。它抑制乙酰胆碱酯酶(IC50=4.15 µM)和丁酰胆碱酯酶(IC50=37 nM)。
Nature, 2018, 560(7718):372-376
S4776 Harmaline Harmaline, a natural occurrence β-carboline alkaloid, is a central nervous system stimulant and an acetylcholinesterase (AChR) inhibitor; also inhibits histamine N-methyltransferase.
S3903 Lycorine Lycorine (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.
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)是一种抗毒蕈碱类的抗帕金森病药物。
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 是一种烟碱受体抑制剂,用作解痉药。
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.
S0016 SN-6 SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3,对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。
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.
Neurotherapeutics, 2021, 10.1007/s13311-021-01052-3
S9560 Anisodamine Hydrobromide Anisodamine (6-Hydroxyhyoscyamine)是天然存在的阿托品(atropine)衍生物,具有消炎活性。它能抑制α1-adrenergic receptorsmAChRs
S4838 Acotiamide hydrochloride Acotiamide Hydrochloride (YM-443, Z-338)是acotiamide的盐酸形式,acotiamide是一种肠蠕动促进剂。它是一种新型的、具有口服活性的、选择性的AChE抑制剂。
S9179 Catharanthine hemitartrate Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine.
S5493 Atropine sulfate Atropine Sulfate (Sulfatropinol, Atropette, Tropintran) is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects.
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S4575 Pralidoxime chloride Pralidoxime chloride (2-PAM)是有机磷农药和一些化学制品的解毒剂。是AChE的重新激活剂。
S5100 Pralidoxime Iodide Pralidoxime Iodide (2-PAM)是一种解毒剂,有机磷中毒后可重新激活被抑制的AChE。
S4389 Bephenium Hydroxynaphthoate Bephenium 是一种 B-type Acetylcholine receptor (AChR) 的激活剂。Bephenium 可选择性地激活由Hco-UNC-29.1,Hco-UNC-38,Hco-UNC-63,Hco-ACR-8亚基组成的Hco-L-AChR1亚型。Bephenium hydroxynaphthoate 是一种驱虫药,以前用于治疗钩虫感染和蛔虫病。
S2547 Tiotropium Bromide hydrate Tiotropium Bromide hydrate (BA 679BR)是Tiotropium bromide (Spiriva; Tiova; BA 679BR; Tiopropium)的一水合物,是抗胆碱药,支气管扩张剂及毒蕈碱受体拮抗剂。
S2497 Pancuronium dibromide Pancuronium dibromide是一种竞争性的乙酰胆碱受体拮抗剂,用作肌肉松弛剂。
Elife, 2019, 8e45399
Front Physiol, 2019, 10:1039
Scholars' Bank, 2019, N/A
E0829New Nitrocaramiphen hydrochloride Nitrocaramiphen hydrochloride是毒蕈碱乙酰胆碱受体 M1 (muscarinic acetylcholine receptor M1, mAChR M1)的拮抗剂,可完全消除毒蕈碱的超极化作用。
S2550 Tolterodine tartrate Tolterodine tartrate (PNU-200583E)是Tolterodine的酒石酸盐形式,是一种竞争性的毒蕈碱型乙酰胆碱受体拮抗剂。
JCI Insight, 2019, 4(20)
S2240 Fesoterodine Fumarate Fesoterodine Fumarate (SPM 907) 是毒蕈碱受体拮抗剂5-羟甲基托特罗定的前药,用来治疗膀胱过度活动症。
Hum Mol Genet, 2020, ddaa244
S1754 Oxybutynin Oxybutynin 是一种竞争性的muscarinic acetylcholine receptorM1,M2,和M3拮抗剂,用于减少尿量,减轻膀胱负担。
S3048 Solifenacin succinate Solifenacin succinate (YM905)是一种抗毒蕈碱类泌尿解痉药。
S1683 Ipratropium Bromide Ipratropium bromide是毒蕈碱拮抗剂,支气管扩张剂,是AtropineN的异丙基盐。
Int Forum Allergy Rhinol, 2020, 10(2):233-242
Anal Chem, 2019, 91(18):11888-11896
S2549 Trospium chloride Trospium chloride 是一种竞争性的毒蕈碱型乙酰胆碱受体拮抗剂。
FEBS Lett, 2020, 10.1002/1873-3468.14015
S2130 Atropine sulfate monohydrate Atropine sulfate monohydrate是一种竞争性毒蕈碱型乙酰胆碱受体拮抗剂,IC50为2.5 nM。
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
S1978 Methscopolamine Methscopolamine是一种毒蕈碱型乙酰胆碱受体抑制剂。
Mol Brain, 2021, 14(1):113
Mol Neurobiol, 2020, 10.1007/s12035-020-02175-y
Neuropharmacology, 2019, 146:252-263
S2508 Scopolamine (LSM-4015) HBr Scopolamine HBr (LSM-4015, NSC 61806)是一种竞争性的毒蕈碱型乙酰胆碱受体拮抗剂,IC50为55.3 ± 4.3 nM。
Exp Ther Med, 2020, 20(4):3625-3632
Mol Cell, 2019, 75(1):53-65
Autophagy, 2019, 10.1080/15548627.2019.1630224
S2659 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)是一种新的蕈毒碱受体拮抗剂,Kb为0.84 nM.
S3144 Darifenacin HBr Darifenacin HBr (UK-88525)是一种选择性的M3 muscarinic(M3蕈毒碱)受体拮抗剂,pKi为8.9。
JCI Insight, 2017, 2(3):e89780
S5873 Scopolamine HBr trihydrate Scopolamine HBr是一种竞争性的蕈毒碱型乙酰胆碱受体(muscarinic acetylcholine receptor)拮抗剂,IC50为55.3 nM。
S4931 Propiverine hydrochloride Propiverine是一种抗胆碱能药物,用于治疗膀胱过度活动症和尿失禁。
S0032 Batefenterol  Batefenterol (GSK961081, TD-5959) 既是 muscarinic receptor 的拮抗剂又是 β2-adrenoceptor 的激动剂,hM2、hM3 muscarinic receptors 和 hβ2-adrenoceptor 的Ki值分别为1.4 nM、1.3 nM和3.7 nM。
S4713 Atropine Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) 是一种具有竞争性的 muscarinic acetylcholine receptor (mAChR) 的拮抗剂,具有抗近视作用。
S5480 Clidinium Bromide Clidinium Bromide is an anticholinergic drug.
S4024 Homatropine Methylbromide Homatropine Methylbromide是一种毒蕈碱受体AChR拮抗剂,抑制WKY-E和SHR-E , IC50分别为162.5 nM和170.3 nM。
Nature, 2018, 560(7718):372-376
S6985 Varenicline Varenicline具有高度选择性,对α4β2 receptors的阻断作用比其他烟碱受体高500倍以上,比非烟碱受体和转运蛋白高2000倍以上。Varenicline 还可作为5-HT3 serotonine receptors的激动剂。
S4025 Homatropine Bromide Homatropine Bromide是一种毒蕈碱受体AChR拮抗剂,抑制WKY-E和SHR-E , IC50分别为162.5 nM和170.3 nM。
S4027 Flavoxate HCl Flavoxate (NSC-114649)是一种毒蕈碱受体AChR拮抗剂, IC50为12.2 μM.
S5238 Solifenacin (YM905) Solifenacin (YM905) is a competitive muscarinic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle.
S5258 Revefenacin Revefenacin (TD-4208, 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 是一种骨骼肌松弛剂,作用于中枢神经系统,产生肌肉松弛作用。
S4034 Diphemanil Methylsulfate Diphemanil Methylsulfate是一种季铵抗胆碱能药剂,可以结合毒蕈碱型乙酰胆碱受体(mAchR)。
S4143 Pentoxyverine Citrate Pentoxyverine Citrate (Carbetapentane) 是antitussive(止咳药),通常用于治疗咳嗽相关的疾病,如感冒。
S5777 Ipratropium bromide monohydrate Ipratropium bromide (Atrovent, Sch 1000) monohydrate 是 muscarinic acetylcholine receptors (mAChR) 的拮抗剂,对M1、M2和M3受体的IC50值分别为2.9 nM、2.0 nM和1.7 nM。
S3701 Benactyzine hydrochloride Benactyzine hydrochloride是中枢性毒蕈碱受体拮抗剂。在抑郁症和相关焦虑的治疗中,它被用作抗抑郁剂。
S5699 Scopolamine N-Oxide HydrobroMide Monohydrate Scopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine)是毒蕈碱拮抗剂,用于研究m型胆碱能受体的结合特性。
S4623 Methylbenactyzine Bromide Methylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) 是一种毒蕈硷胆碱能受体拮抗剂,具有解痉活性。
S4069 Hexamethonium Dibromide Hexamethonium Dibromide是一种神经中枢中选择性的神经元烟碱型AChR选择性拮抗剂。
S4660 Glycopyrrolate Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn)是毒蕈碱拮抗剂。在胃肠道疾病中,被用作止痉挛药。
J Clin Med, 2022, 11(9)2307
S3735 Umeclidinium bromide Umeclidinium bromide是一种长效毒蕈碱拮抗剂,对治疗慢性阻塞性肺疾病具有持续性疗效。
S5538 Tropisetron Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
S3117 Oxybutynin hydrochloride Oxybutynin chloride是一种抗胆碱药,用于缓解尿和膀胱负担。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
S4834 Propantheline bromide Propantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan)是一种毒蕈碱拮抗剂,用于治疗和肠痉挛相关的胃肠道疾病、在麻醉过程中减少分泌。
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) 是抗组胺剂和抗胆碱能药。
S3298 Caulophylline (N-Methylcytisine) Caulophylline (N-Methylcytisine, Caulophyllin, NMC) 是一种具有抗炎活性的三环喹喔啉生物碱。Caulophylline 可与鱿鱼视神经节的 nicotinic acetylcholine receptors (nAChR) 结合,Kd值为50 nM。Caulophylline 可显著地降低 myeloperoxidase (MPO) 的活性,并通过抑制 IκBIKK 磷酸化来阻断 NF-κB 的活化。
S5921 Cyclopentolate Hydrochloride Cyclopentolate是毒蝇碱型乙酰胆碱受体拮抗剂,对M1、M2和M3受体的Ki值分别为1.62, 27.5和2.63 nM。
S4292 Diphenidol HCl Diphenidol HCl是一种有效的muscarinic M2 and M3 receptor拮抗剂,pKb分别为6.72和7.02,用于呕吐和晕眩的治疗。
S0702 α-Conotoxin GI α-ConotoxinGI最初是从鸡心螺的猎鱼毒液中分离出来的13残基肽,作为肌肉型烟碱型乙酰胆碱受体(Nicotinic acetylcholine receptors, nAChRs)的竞争性拮抗剂,相对α/γ来说,对α/δ受体亚单位结合具有极好的选择性。
S1913 Tropicamide Tropicamide是一种抗胆碱,毒蕈碱受体M4亚型的选择性拮抗剂,IC50为8.0 nM。
S1356 Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) 是一种抗癫痫化合物。Levetiracetam (UCB-L059, SIB-S1) 是 muscarinic acetylcholine receptors (mAChR) 的激动剂并能调节突触前P/Q型压敏钙离子通道 calcium (Ca2+) channel
Anticancer Res, 2021, 41(2):687-697
PLoS One, 2019, 14(2):e0211644
Sci Rep, 2016, 6:25705
E1265New Deschloroclozapine Deschloroclozapine,Clozapine的一种代谢物,是一种高效的毒蕈碱型设计药物激活专门受体(muscarinic Designer Receptors Exclusively Activated by Designer Drugs, muscarinic DREADD)激动剂,与DREADD的受体亚型hM3Dq和hM4Di结合,Ki分别为6.3和4.2 nM。
E0755New Guvacoline hydrochloride Norarecoline hydrochloride (Guvacoline hydrochloride)是一种在槟榔(Areca triandra)中发现的吡啶类生物碱,可作为心房和回肠毒蕈碱受体的完全激动剂。
E0176New Dinotefuran Dinotefuran (MTI-446) 作为一种新烟碱类化合物,是一种有效的 nAChRs 激动剂,EC50 为 7.8 μM,对 Da2b2 杂合 nAChRs 显示出高杀虫活性。
E0172New Imidacloprid Imidacloprid是一种烟碱型乙酰胆碱受体 (nAChR) 激动剂,具有强效杀虫活性。
S1440 Varenicline Tartrate (CP 526555-18) Varenicline Tartrate (CP 526555-18, Chantix, Champix)是一种烟碱类AChR激动剂,用于治疗吸烟成瘾。
S2455 Bethanechol chloride Bethanechol chloride是一种选择性毒蕈碱受体激动剂,对烟碱受体没有任何效果。
Environ Toxicol Chem, 2021, 10.1002/etc.5018
Exp Physiol, 2020, 10.1113/EP088900
Lung, 2018, 196(2):219-229
S2614 Arecoline HBr Arecoline是一种毒蕈碱型乙酰胆碱受体激动剂。
Oncogene, 2020, 39(11):2437-2449
BMC Mol Cell Biol, 2020, 21(1):80
Oncol Rep, 2015, 33(6):2753-60
S4231 Pilocarpine HCl Pilocarpine HCl (NSC 5746)是非选择性毒蕈碱型乙酰胆碱受体激动剂,用于产生癫痫的实验模型。
Theranostics, 2021, 11(12):5986-6005
Mol Brain, 2021, 14(1):113
Anticancer Res, 2021, 41(2):687-697
S0717 Varenicline (CP 526555) dihydrochloride Varenicline (CP 526555) dihydrochloride 是 α4β2 nicotinic acetylcholine receptor (nAChR)α3β4 nAChR 的有效部分激动剂,EC50分别为2.3 μM和55 μM。Varenicline dihydrochloride 是一种有效的 α7 nAChRs 的完全激动剂,EC50值为18 μM。Varenicline 是可用于戒烟的处方药。
S0720 PNU-282987 PNU-282987 是一种新型的 alpha7 nAChR 选择性激动剂,对大鼠 alpha7 nAChR 的 Ki 为 26 nM。除了 Ki 为 930 nM 的 5-HT3 受体外,PNU-282987 对所有测试的单胺、毒蕈碱、谷氨酸和 GABA 受体均无活性。
S0728 N-Desmethylclozapine N-Desmethylclozapine (Norclozapine, Normethylclozapine), a metabolite of the atypical antipsychotic drug Clozapine, is a potent, allosteric and partial agonist of M1 receptors with EC50 of 115 nM. N-Desmethylclozapine is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation and also a δ-opioid agonist.
S0740 PNU-282987 S enantiomer hydrochloride (S)-PNU-282987 is the absolute stereochemistry form of PNU-282987. PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors (nAChRs) with Ki of 26 nM for the rat receptor. PNU 282987 has negligible activity against α1β1γδ and α3β4 nAChRs as well as a panel of monoamine, muscarinic, glutamate, and GABA receptors, except 5-HT3 with Ki of 930 nM.
S4121 Succinylcholine Chloride Dihydrate Succinylcholine Chloride Dihydrate (Suxamethonium)是一种烟碱AChR激动剂,同时也是一种去极化神经肌肉阻断剂。
S4422 Nitenpyram Nitenpyram是一个nicotinic acetylcholine receptor (AchR)激动剂,用于兽医对家畜和宠物寄生虫的治疗。
Proc Natl Acad Sci U S A, 2020, 117(21):11321-11327
S7366 LY2119620 LY2119620是一种人类M2 and M4 muscarinic acetylcholine receptors的特异变构激动剂。
S2287 Cytisine Cytisine (Baphitoxine, Sophorine)是一种烟碱型乙酰胆碱受体激动剂。
S4171 Choline Chloride Choline chloride是一种季铵盐,作为动物饲料添加剂。它是acetylcholine的前体化合物,在多种代谢过程、脂质代谢中作为甲基供体。
S4072 Decamethonium Bromide Decamethonium Bromide是一种烟碱AChR部分激动剂和神经肌肉阻断剂。
S9789 JHU37152 JHU37152 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq)hM4Di 的Ki值分别为1.8 nM和8.7 nM。在HEK-293细胞中基于荧光和BRET的检测中,对 hM3Dq 和 hM4Di 的EC50值分别为5 nM和0.5 nM。
S9790 JHU37160 JHU37160 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq)hM4Di 的Ki值分别为1.9 nM和3.6 nM。在HEK-293细胞中基于荧光和BRET的检测中,对 hM3Dq 和 hM4Di 的EC50值分别为18.5 nM和0.2 nM。
S6432 Cevimeline Cevimeline (AF 102B, SNI 2011, SNK 508)是一种拟副交感神经药,是毒蕈碱样乙酰胆碱受体M1和M3的激动剂。
S6887 Clozapine N-oxide Clozapine N-oxide (CNO) 是一种 Clozapine (GLXC-06516) 的代谢产物,是 human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs) 的激动剂。Clozapine 是一种有效的 dopamine (DA) 拮抗剂和选择性的 muscarinic M4 receptor 的激动剂。
S3684 Methacholine chloride Methacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors.
S5930 PNU 282987 HCl PNU 282987是一种有效的含α7的神经元烟碱受体(α7-containing neuronal nicotinic acetylcholine receptors)激动剂,对大鼠受体的Ki值为26 nM。
S4359 Carbamoylcholine chloride (Carbachol) Carbamoylcholine chloride (Carbachol, Carbamylcholine chloride, Carbastat, Miostat) 是一种 cholinergic 胆碱能的激动剂,模仿乙酰胆碱对 muscarinic and nicotinic receptors 的作用。
S2957 Encenicline (EVP-6124) hydrochloride Encenicline (EVP-6124) hydrochloride是一种选择性α7烟碱型乙酰胆碱受体(α7 nicotinic acetylcholine receptor, α7 nAChR)部分激动剂,通过增强α7烟碱型乙酰胆碱受体的乙酰胆碱反应来提高记忆力。
S0457 DREADD agonist 21 DREADD agonist 21 是一种有效的 human muscarinic acetylcholine M3 receptors (hM3Dq) 激动剂,其EC50值为1.7 nM。
S1805 Acetylcholine Chloride 化合物Acetylcholine Chloride是一种神经递质,作用于包括人类在内的许多生物的周围神经系统(PNS)和中枢神经系统(CNS)。
Biotechnol Lett, 2020, 42(7):1219-1227
Med Sci Monit, 2019, 25:5389-5400
S4718 Acetylcholine iodide Acetylcholine iodide (Acetylcolina)是一种存在于肌肉神经接点、自主神经节、副交感效应连接处以及中枢神经系统很多地方的神经递质。
Biotechnol Lett, 2020, 42(7):1219-1227
S6795 VU0357017 Hydrochloride VU0357017 hydrochloride (CID-25010775)是一种强效的、中枢神经系统渗透性的高选择性 M1 激动剂,M1是 muscarinic acetylcholine receptors (mAChRs) 的一类亚型。VU0357017 hydrochloride 可在变构位点起作用以激活该受体,其EC50值为 477 nM 和 Ki值为 9.91 μM。
E0799New VU 0365114 VU 0365114 是一种毒蕈碱乙酰胆碱受体M5偏好(muscarinic acetylcholine receptor M5-preferring , mAChR M5-preferring)的正变构调节剂 (positive allosteric modulator, PAM),EC50为2.7 μM。
E0382New W-84 Dibromide W-84 dibromide (HDMPPA)是一种有效的M2-乙酰胆碱受体的变构调节剂,可抑制3HN-甲基多胺的解离。
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) 是一种chloride channel激活剂,用作广谱抗寄生虫药。Ivermectin (MK-933, IVM) 是 P2X4α7 nicotinic acetylcholine receptors (nAChRs) 的特异性正变构效应物。Ivermectin 对 HIV-1 和登革热dengue virus均具有有效的抗病毒活性。Ivermectin 可通过AKT/mTOR信号通路来诱导自噬,并诱导线粒体自噬。
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
S2629 PNU-120596 PNU-120596 (Nsc 216666)是一种有效的α7 nAChR变构调节剂,EC50为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
S0518 NS 1738 NS 1738 (NSC 213859)是一种新型的α7烟碱乙酰胆碱受体(α7 nicotinic acetylcholine receptor, α7 nAChR)正变构调节剂,对非洲蟾卵卵母细胞α7 nAChR具有正向调节作用,EC50为3.4 μM,对大鼠α7 nAChR具有相当的调节作用,EC50为3.9 μM。
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
S0552 BNC210 BNC210 (H-Ile-Trp-OH, IW-2143) 是一种 alpha-7 nicotinic acetylcholine receptor (α7 nAChR) 的负变构调节剂。
S0782 VU0238441 VU0238441 是一种泛 muscarinic acetylcholine receptor (mAChR) 的正向变构调节剂 (PAM),对于M5、M3、M2、M1和M4的EC50值分别为2.1 μM、2.2 μM、2.8 μM、3.2 μM 和 >10 μM。
S0783 VU0119498 VU0119498 是一种泛Gq muscarinic acetylcholine receptor (mAChR) M1,M3,M5的正向变构调节剂(PAM),对应EC50值分别为6.1 μM, 6.4 μM, 4.1 μM。
S5931 BQCA BQCA (benzylquinolone carboxylic acid)是一种高选择性M1 muscarinic acetylcholine receptor (mAChR)正向别构调节剂。
S5844 Lobelin sulphate Lobelin sulphate (Lobeline sulfate, Bantron) 对烟碱性胆碱能受体具有与尼古丁类似的作用。它应用于多种疾病的治疗,如呼吸道疾病、周围性血管疾病、失眠症以及戒烟过程。
S5747 Morantel tartrate Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).
S2646 VU0238429 VU0238429 (M5 PAM)是第一个 muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) 的阳性变构调节剂,对于M5的EC50值为 1.16 μM,而对于M1和M3的EC50均大于 30 μM。VU0238429 对于M2和M4没有显现出增强剂的活性。
E0831New Pseudocoptisine chloride Pseudocoptisine chloride (Isocoptisine chloride)是一种分离自Corydalis Tuber具有苄基异喹啉骨架的季生物碱,抑制乙酰胆碱酯酶(acetylcholinesterase, AChE)活性,IC50为12.8 μM,具有抗炎和抗健忘的作用。
E0829New Nitrocaramiphen hydrochloride Nitrocaramiphen hydrochloride是毒蕈碱乙酰胆碱受体 M1 (muscarinic acetylcholine receptor M1, mAChR M1)的拮抗剂,可完全消除毒蕈碱的超极化作用。
E1265New Deschloroclozapine Deschloroclozapine,Clozapine的一种代谢物,是一种高效的毒蕈碱型设计药物激活专门受体(muscarinic Designer Receptors Exclusively Activated by Designer Drugs, muscarinic DREADD)激动剂,与DREADD的受体亚型hM3Dq和hM4Di结合,Ki分别为6.3和4.2 nM。
E0755New Guvacoline hydrochloride Norarecoline hydrochloride (Guvacoline hydrochloride)是一种在槟榔(Areca triandra)中发现的吡啶类生物碱,可作为心房和回肠毒蕈碱受体的完全激动剂。
E0176New Dinotefuran Dinotefuran (MTI-446) 作为一种新烟碱类化合物,是一种有效的 nAChRs 激动剂,EC50 为 7.8 μM,对 Da2b2 杂合 nAChRs 显示出高杀虫活性。
E0172New Imidacloprid Imidacloprid是一种烟碱型乙酰胆碱受体 (nAChR) 激动剂,具有强效杀虫活性。
E0799New VU 0365114 VU 0365114 是一种毒蕈碱乙酰胆碱受体M5偏好(muscarinic acetylcholine receptor M5-preferring , mAChR M5-preferring)的正变构调节剂 (positive allosteric modulator, PAM),EC50为2.7 μM。
E0382New W-84 Dibromide W-84 dibromide (HDMPPA)是一种有效的M2-乙酰胆碱受体的变构调节剂,可抑制3HN-甲基多胺的解离。
E0524New Spinosad Spinosad是一种具有更广泛作用谱的生物神经毒性杀虫剂,是一种由spinosyns A和D混合而成的,是一种土壤放线菌发酵产物,Spinosad靶向昆虫神经系统的烟碱乙酰胆碱受体 (nicotinic acetylcholine receptor,nAChRs)
Tags: AChR inhibitor|AChR agonist|AChR activator|AChR inducer|AChR antagonist|AChR signaling pathway|AChR assay kit