S4505 |
Vinblastine sulfate
|
Vinblastine sulfate抑制微管形成和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。 |
-
Int J Mol Sci, 2024, 25(21)11346
-
PLoS One, 2024, 19(11):e0307153
-
Nat Commun, 2023, 14(1):7576
|
|
S1351 |
Ivermectin
|
Ivermectin是一种chloride channel激活剂,用作广谱抗寄生虫药。Ivermectin (MK-933, IVM) 是 P2X4 和 α7 nicotinic acetylcholine receptors (nAChRs) 的特异性正变构效应物。Ivermectin (MK-933) 是一种特异性的 Impα/β1 介导的核导入抑制剂,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。 |
-
Viruses, 2024, 16(4)640
-
Life Sci Alliance, 2023, 6(8)e202302133
-
Cell Rep Methods, 2023, 3(10):100599
|
|
S2462 |
Donepezil HCl
|
Donepezil HCl 是一种特异性的,有效的AChE抑制剂,作用于bAChE和hAChE,IC50分别为8.12 nM和11.6 nM。此产品不溶于PBS,请勿用PBS溶解给药。 |
-
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)是一种有效的α7 nAChR变构调节剂,EC50为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)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。 |
-
Viruses, 2024, 16(10)1559
-
Heliyon, 2024, 10(1):e23945
-
Theranostics, 2021, 11(12):5986-6005
|
|
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。 |
-
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)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。 |
-
Heliyon, 2024, 10(1):e23945
-
Zool Res, 2023, 44(4):712-724
-
Zool Res, 2023, 44(4):712-724
|
|
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 nAChRs和α7 nAChRs,IC50分别为49 nM 和 122 nM。 |
-
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) 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。 |
-
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)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。在溶液中不稳定,请现配现用! |
-
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)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
-
G3 (Bethesda), 2014, 10.1534/g3.114.010819
|
|
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。 |
-
Theranostics, 2023, 13(6):1826-1842
-
Front Bioeng Biotechnol, 2022, 10:855755
-
Front Cardiovasc Med, 2021, 8:639541
|
|
S1805 |
Acetylcholine Chloride
|
化合物Acetylcholine Chloride(ACh 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)。 |
-
Cell Mol Life Sci, 2024, 81(1):88
-
iScience, 2023, 26(3):106241
-
Cell, 2022, 185-21:3950-3965.e25
|
|
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
|
|
S2455 |
Bethanechol chloride
|
Bethanechol chloride(Myocholine,Urecholine)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(NSC-31750)是一种毒蕈碱型乙酰胆碱受体激动剂。 |
-
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
|
|
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。 |
-
Neurosci Bull, 2023, none
-
Neurochem Res, 2020, 10.1007/s11064-020-03103-1
|
|
S3047 |
Otilonium Bromide
|
Otilonium Bromide是一种抗毒蕈碱药物. |
-
Biochem Pharmacol, 2023, 215:115746
-
Res Microbiol, 2022, S0923-2508(22)00073-0
|
|
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。 |
-
J Cell Physiol, 2023, 10.1002/jcp.31057
-
Mol Psychiatry, 2018, 23(3):767-776
|
|
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。 |
-
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) 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
|
|
S4171 |
Choline Chloride
|
Choline chloride(Hepacholine)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。 |
-
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)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。 |
-
Food Sci Nutr, 2022, 10(8):2773-2785
-
Biotechnol Lett, 2020, 42(7):1219-1227
|
|
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
|
|
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。 |
-
Neuropharmacology, 2023, S0028-3908(23)00262-9
|
|
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。 |
-
J Cell Physiol, 2023, 10.1002/jcp.31057
|
|
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
|
|
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
|
|
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
|
|
S4014 |
Hyoscyamine
|
Hyoscyamine (Daturine) 是一种AChR抑制剂,IC50为7.5nM。 |
-
Theranostics, 2022, 12(12):5488-5503
|
|
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。 |
-
iScience, 2023, 26(3):106241
|
|
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
|
|
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。 |
-
Cell Rep Methods, 2023, 3(10):100599
|
|
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。 |
-
Int J Mol Sci, 2023, 10.3390/ijms242115535
|
|
S4422 |
Nitenpyram
|
Nitenpyram(Bestguard,Capstar)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
|
|
S2287 |
Cytisine
|
Cytisine (Baphitoxine, Sophorine)是一种烟碱型乙酰胆碱受体激动剂。 |
-
Transl Oncol, 2023, 35:101712
|
|
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
|
|
S6432 |
Cevimeline HCl hemihydrate
|
Cevimeline HCl hemihydrate(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。 |
-
Front Pharmacol, 2022, 13:914153
|
|
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
|
|
S3117 |
Oxybutynin hydrochloride
|
Oxybutynin chloride(MJ4309-1)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
|
|
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)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。 |
|
|
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。 |
-
J Immunother Cancer, 2024, 12(11)e009805
|
|
S1405 |
Vecuronium Bromide
|
Vecuronium Bromide (ORG NC45) 是一种肌肉松弛剂,属于非去极化抑制剂。 |
|
|
S2378 |
Butylscopolamine Bromide
|
Butylscopolamine Bromide (Scopolamine Butylbromide,(-)-Scopolamine butylbromide, Hyoscine butylbromide)是一种外周性的抗毒蕈碱,抗胆碱的药剂,用作腹部特定的解痉药。 |
|
|
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。 |
|
|
S1929 |
Irsogladine
|
Irsogladine(Dicloguamine)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。 |
|
|
E0524 |
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)。 |
|
|
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。 |
|
|
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。 |
|
|
S0717 |
Varenicline (CP 526555) dihydrochloride
|
Varenicline (CP 526555) dihydrochloride 是 α4β2 nicotinic acetylcholine receptor (nAChR) 和 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。 |
|
|
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。 |
|
|
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。 |
|
|
S3245 |
Nodakenetin
|
Nodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素,可抑制 α-glucosidase、PTP1B、rat lens aldose reductase (RLAR)、AChE、BChE 和 β-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 Bax 和 Bcl-2 的蛋白质表达,并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。 |
|
|
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。 |
|
|
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。 |
|
|
E3551 |
Stephania Extract
|
Stephania Extract从千金藤Stephania中提取,通过抑制乙酰胆碱酯酶和氧化应激改善东莨菪碱诱导的小鼠记忆障碍。 |
|
|
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是PNU-282987 free base的S-对映体,PNU-282987 free base是一种α7烟碱乙酰胆碱受体(α7 nicotinic acetylcholine receptor, α7 nAChR)激动剂。 |
|
|
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。 |
|
|
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。 |
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S3246 |
Picfeltarraenin IB
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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。 |
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S5480 |
Clidinium Bromide
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Clidinium Bromide(Ro 2-3773) is an anticholinergic drug. |
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S5385 |
Imidafenacin
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Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3). |
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S6985 |
Varenicline
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Varenicline(CP 526555)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。 |
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S4025 |
Homatropine Bromide
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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。 |
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E4822New |
Tacrine
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Tacrine是一种有效的acetylcholinesterase (AChE)和butyrylcholinesterase (BChE)抑制剂, IC50分别为77 nM和69 nM,用于治疗阿尔茨海默病,也可抑制拓扑异构酶和mtDNA的合成。 |
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S4027 |
Flavoxate HCl
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Flavoxate (NSC-114649)是一种毒蕈碱受体AChR拮抗剂, IC50为12.2 μM. |
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S9326 |
Scopolamine
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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. |
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Immunity, 2024, 57(2):364-378.e9
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S5238 |
Solifenacin (YM905)
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Solifenacin (YM905) is a competitive muscarinic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle. |
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S3820 |
Dehydroevodiamine hydrochloride
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Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production. |
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S5258 |
Revefenacin
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Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease. |
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S2054 |
Orphenadrine Citrate
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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。 |
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E0172 |
Imidacloprid
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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。 |
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S4034 |
Diphemanil Methylsulfate
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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)。 |
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E3651 |
Lycopodiastrum casuarinoides Extract
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Lycopodiastrum casuarinoides Extract是从舒筋草Lycopodiastrum casuarinoides中提取的,具有乙酰胆碱酯酶抑制活性。 |
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S9252 |
Corydaline
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Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
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S1832 |
Atracurium Besylate
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Atracurium Besylate (BW 33A, 51W89)是一种神经肌肉抑制剂,ED95为0.2 mg/kg。 |
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S0552 |
BNC210
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BNC210 (H-Ile-Trp-OH, IW-2143) 是一种 alpha-7 nicotinic acetylcholine receptor (α7 nAChR) 的负变构调节剂。 |
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S0766 |
RHC 80267
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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。 |
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S9260 |
Nodakenin
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Nodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM. |
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S5022 |
Varenicline Hydrochloride
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Varenicline (CP 526555) Hydrochloride 是 α4β2 尼古丁乙酰胆碱受体 (nicotine acetylcholine receptor, nAChR) 和 α6β2 尼古丁乙酰胆碱受体 (nAChR) 的部分激动剂,Ki 值为 0.12 nM 和 0.14 大鼠纹状体中的 α6β2 nAChR 和 α4β2 nAChR 分别为 nM。 |
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S4143 |
Pentoxyverine Citrate
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Pentoxyverine Citrate (Carbetapentane) 是antitussive(止咳药),通常用于治疗咳嗽相关的疾病,如感冒。 |
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S3835 |
Loganin
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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
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Desmethylanethol trithione (ADT-OH)是anethole dithiolethione (ADT)的衍生物,是合成的硫化氢 (H2S)供体。 |
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F2495New |
Acetylcholinesterase Rabbit mAb
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E3116 |
Acanthopanax Senticosus Extract
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Acanthopanax Senticosus Extract提取自刺五加Acanthopanax Senticosus,对小鼠回肠功能具有通过毒蕈碱乙酰胆碱受体(mAChRs)收缩和直接弛缓的双重作用,其弛缓作用可用于治疗腹泻症状,使副交感神经活性增加。 |
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S4619 |
Itopride hydrochloride
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Itopride hydrochloride (Ganaton, HSR803) 是一种AChE抑制剂。其IC50为2.04 +/- 0.27 μM。 |
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E1876New |
GTS-21 dihydrochloride
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GTS-21 dihydrochloride(DMXB-A, DMBX-anabaseine)是 α7 烟碱型乙酰胆碱受体 (α7-nAChR) 的选择性激动剂,具有抗炎和认知增强活性。 GTS-21 diHClide 也是 α4β2 的拮抗剂,对人 α4β2 的 Ki 值为 20 nM,对 5-HT3A 受体 的 IC50 值为 3.1 μM。 |
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S0782 |
VU0238441
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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。 |
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S0783 |
VU0119498
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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。 |
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S5777 |
Ipratropium bromide monohydrate
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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。 |
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S7366 |
LY2119620
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LY2119620是一种人类M2 and M4 muscarinic acetylcholine receptors的特异变构激动剂。
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S9459 |
Mecamylamine Hydrochloride
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Mecamylamine hydrochloride是一种口服活性、非选择性、非竞争性nAChR(烟碱型乙酰胆碱受体)拮抗剂。它也是一种神经节阻滞剂,可以穿过血脑屏障。 可用于神经精神疾病、高血压、抗抑郁领域的研究。 |
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E3612 |
Cremastra appendiculata Extract
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Cremastra Appendiculata Extract来源于山慈菇 Cremastra appendiculata (Pseudobulbus Cremastrae seu Pleiones)。山慈姑是兰科植物的干燥假鳞茎。山慈菇具有抗菌、抗高血压、治疗痛风、抗肿瘤和乙酰胆碱受体M3阻断作用。山慈菇提取物可用于治疗肺癌、肝癌和乳腺癌。 |
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E0829 |
Nitrocaramiphen hydrochloride
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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。 |
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E2874 |
Sofpironium bromide
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Sofpironium bromide(BBI 4000)是一种抗胆碱化合物,通过抑制汗腺中的M3毒蕈碱受体,减少汗液分泌。 |
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E0755 |
Guvacoline hydrochloride
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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。 |
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E4714New |
Xanomeline
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Xanomeline(LY-246708) 是毒蕈碱型 1(M(1) 受体 和 毒蕈碱型 4 受体(M(4) ) 的选择性激动剂。它能增加神经元兴奋性,抑制 D-苯丙胺和 (-)-阿扑吗啡诱发的行为。 |
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S3701 |
Benactyzine hydrochloride
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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。 |
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S5699 |
Scopolamine N-Oxide HydrobroMide Monohydrate
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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。 |
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S3913 |
Pimethixene maleate
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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。 |
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E3223 |
Alpiniae Officinarum Rhizoma Extract
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Alpiniae Officinarum Rhizoma Extract从高良姜Alpiniae Officinarum Rhizoma中提取,对乙酰胆碱酯酶(AChE)有抑制作用,可用于治疗阿尔茨海默病。 |
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S4623 |
Methylbenactyzine Bromide
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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。 |
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E0799 |
VU 0365114
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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。 |
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E4298 |
(-)-Carvone
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(-)-Carvone是一种昆虫神经毒素,是乙酰胆碱酯酶 (AChE) 的不可逆抑制剂。 可用作驱鸟剂,抑制幼虫生长,降低化蛹率,增加幼虫死亡率。 |
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S3639 |
Tacrine hydrochloride hydrate
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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。 |
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S4069 |
Hexamethonium Dibromide
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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。 |
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S4072 |
Decamethonium Bromide
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Decamethonium Bromide是一种烟碱AChR部分激动剂和神经肌肉阻断剂。 |
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S3662 |
Pirenzepine dihydrochloride
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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. |
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S9789 |
JHU37152
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JHU37152 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq) 和 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。 |
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S9790 |
JHU37160
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JHU37160 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq) 和 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。 |
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E1265 |
Deschloroclozapine
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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。 |
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S3311 |
Myosmine
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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。 |
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S3769 |
Palmatine
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Palmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities. |
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Eur J Pharmacol, 2024, 967:176395
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E0382 |
W-84 Dibromide
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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。 |
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S9069 |
Jatrorrhizine chloride
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Jatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
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S5850 |
Vasicine
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Vasicine,可分离自A. vasica,是一种生物碱。它是天然的cholinesterase(胆碱酯酶)抑制剂,在临床前模型中具有抗胆碱酯酶活性,可用于阿尔茨海默病的治疗药物开发。 |
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S3788 |
Carvacrol
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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. |
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S9087 |
Tenuifolin
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Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
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S4804 |
1-Naphthyl acetate
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1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages. |
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S3884 |
Jatrorrhizine
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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. |
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S3684 |
Methacholine chloride
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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. |
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S4703 |
Choline bitartrate
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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。 |
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S5930 |
PNU 282987 HCl
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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。 |
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S5931 |
BQCA
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BQCA (benzylquinolone carboxylic acid)是一种高选择性M1 muscarinic acetylcholine receptor (mAChR)正向别构调节剂。 |
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S3735 |
Umeclidinium bromide
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Umeclidinium bromide(GSK573719A)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。 |
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S5538 |
Tropisetron
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Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
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Chin Med, 2024, 19(1):87
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Neural Regen Res, 2023, 18(9):2019-2028
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S5075 |
Acotiamide
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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。 |
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S4357 |
Tacrine HCl
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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. |
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S4359 |
Carbamoylcholine chloride (Carbachol)
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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。此产品为危化品(急性毒性/易燃/皮肤腐蚀),请在穿戴防护面罩、防护手套和防护服后使用。 |
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S2957 |
Encenicline (EVP-6124) hydrochloride
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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。 |
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E0176 |
Dinotefuran
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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。 |
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E0831 |
Pseudocoptisine chloride
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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。 |
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E2237 |
Vasicine (hydrochloride)
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Vasicine hydrochloride(Peganine hydrochloride)是一种从Adhatoda vasica中分离出来的生物碱vasicine (VAS)的盐,是一种潜在的天然胆碱酯酶抑制剂。VAS抑制乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)。 |
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S3904 |
Isoimperatorin
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Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. |
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S4834 |
Propantheline bromide
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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。 |
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S9138 |
Picfeltarraenin IA
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Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system. |
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S4542 |
Trihexyphenidyl hydrochloride
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Trihexyphenidyl hydrochloride (Benzhexol, Artane)是一种抗毒蕈碱类的抗帕金森病药物。 |
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S5511 |
Ethyl (triphenylphosphoranylidene) acetate
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Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
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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. |
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S6469 |
Thonzylamine
|
Thonzylamine (Neohetramine) 是抗组胺剂和抗胆碱能药。 |
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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。 |
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S2082 |
Adiphenine HCl
|
Adiphenine HCl(NSC 129224) 是一种烟碱受体抑制剂,用作解痉药。 |
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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. |
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S9475 |
Hupehenine
|
Hupehenine是来源于湖北贝母鳞茎的甾体生物碱,具有抑制乙酰胆碱、拮抗毒蕈碱性受体、抑制胆碱酯酶的潜力。 |
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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。 |
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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。 |
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S4389 |
Bephenium Hydroxynaphthoate
|
Bephenium(NSC 759245) 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。 |
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S5747 |
Morantel tartrate
|
Morantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs). |
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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 IκB 和 IKK 磷酸化来阻断 NF-κB 的活化。 |
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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 receptors和mAChRs。 |
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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。 |
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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。 |
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S9179 |
Catharanthine hemitartrate
|
Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
|
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S4292 |
Diphenidol HCl
|
Diphenidol HCl(Diphenidol hydrochloride)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。
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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。 |
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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。 |
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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。 |
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S1913 |
Tropicamide
|
Tropicamide(Ro 1-7683)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。 |
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S4505 |
Vinblastine sulfate
|
Vinblastine sulfate抑制微管形成和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。 |
- Int J Mol Sci, 2024, 25(21)11346
- PLoS One, 2024, 19(11):e0307153
- Nat Commun, 2023, 14(1):7576
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S2462 |
Donepezil HCl
|
Donepezil HCl 是一种特异性的,有效的AChE抑制剂,作用于bAChE和hAChE,IC50分别为8.12 nM和11.6 nM。此产品不溶于PBS,请勿用PBS溶解给药。 |
- Theranostics, 2023, 13(6):1826-1842
- J Cell Physiol, 2023, 10.1002/jcp.31057
- Comp Biochem Physiol C Toxicol Pharmacol, 2023, 272:109698
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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 nAChRs和α7 nAChRs,IC50分别为49 nM 和 122 nM。 |
- Nat Commun, 2023, 10.1038/s41467-023-42332-0
- Nat Commun, 2023, 14(1):6690
- iScience, 2023, 26(8):107477
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S2452 |
Amfebutamone (Bupropion) HCl
|
Amfebutamone (Bupropion) HCl(Wellbutrin)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
- G3 (Bethesda), 2014, 10.1534/g3.114.010819
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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。 |
- Theranostics, 2023, 13(6):1826-1842
- Front Bioeng Biotechnol, 2022, 10:855755
- Front Cardiovasc Med, 2021, 8:639541
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S3047 |
Otilonium Bromide
|
Otilonium Bromide是一种抗毒蕈碱药物. |
- Biochem Pharmacol, 2023, 215:115746
- Res Microbiol, 2022, S0923-2508(22)00073-0
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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。 |
- J Cell Physiol, 2023, 10.1002/jcp.31057
- Mol Psychiatry, 2018, 23(3):767-776
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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
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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
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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
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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。 |
- J Cell Physiol, 2023, 10.1002/jcp.31057
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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
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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
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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
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S4014 |
Hyoscyamine
|
Hyoscyamine (Daturine) 是一种AChR抑制剂,IC50为7.5nM。 |
- Theranostics, 2022, 12(12):5488-5503
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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。 |
- Int J Mol Sci, 2023, 10.3390/ijms242115535
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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
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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
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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. |
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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
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S2378 |
Butylscopolamine Bromide
|
Butylscopolamine Bromide (Scopolamine Butylbromide,(-)-Scopolamine butylbromide, Hyoscine butylbromide)是一种外周性的抗毒蕈碱,抗胆碱的药剂,用作腹部特定的解痉药。 |
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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。 |
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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。 |
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S1929 |
Irsogladine
|
Irsogladine(Dicloguamine)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。 |
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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。 |
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S3245 |
Nodakenetin
|
Nodakenetin (NANI) 是从Angelica decursiva中分离出的植物性香豆素,可抑制 α-glucosidase、PTP1B、rat lens aldose reductase (RLAR)、AChE、BChE 和 β-site amyloid precursor protein cleaving enzyme 1 (BACE1)。Nodakenetin 可改变 Bax 和 Bcl-2 的蛋白质表达,并促进线粒体凋亡。Nodakenetin 具有抗肿瘤活性。 |
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E3551 |
Stephania Extract
|
Stephania Extract从千金藤Stephania中提取,通过抑制乙酰胆碱酯酶和氧化应激改善东莨菪碱诱导的小鼠记忆障碍。 |
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S9219 |
Huperzine B
|
Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
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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。 |
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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。 |
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S5385 |
Imidafenacin
|
Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3). |
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E4822New |
Tacrine
|
Tacrine是一种有效的acetylcholinesterase (AChE)和butyrylcholinesterase (BChE)抑制剂, IC50分别为77 nM和69 nM,用于治疗阿尔茨海默病,也可抑制拓扑异构酶和mtDNA的合成。 |
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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. |
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E3651 |
Lycopodiastrum casuarinoides Extract
|
Lycopodiastrum casuarinoides Extract是从舒筋草Lycopodiastrum casuarinoides中提取的,具有乙酰胆碱酯酶抑制活性。 |
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S9252 |
Corydaline
|
Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
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S1832 |
Atracurium Besylate
|
Atracurium Besylate (BW 33A, 51W89)是一种神经肌肉抑制剂,ED95为0.2 mg/kg。 |
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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。 |
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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. |
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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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S4619 |
Itopride hydrochloride
|
Itopride hydrochloride (Ganaton, HSR803) 是一种AChE抑制剂。其IC50为2.04 +/- 0.27 μM。 |
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E3612 |
Cremastra appendiculata Extract
|
Cremastra Appendiculata Extract来源于山慈菇 Cremastra appendiculata (Pseudobulbus Cremastrae seu Pleiones)。山慈姑是兰科植物的干燥假鳞茎。山慈菇具有抗菌、抗高血压、治疗痛风、抗肿瘤和乙酰胆碱受体M3阻断作用。山慈菇提取物可用于治疗肺癌、肝癌和乳腺癌。 |
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E2874 |
Sofpironium bromide
|
Sofpironium bromide(BBI 4000)是一种抗胆碱化合物,通过抑制汗腺中的M3毒蕈碱受体,减少汗液分泌。 |
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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。 |
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E3223 |
Alpiniae Officinarum Rhizoma Extract
|
Alpiniae Officinarum Rhizoma Extract从高良姜Alpiniae Officinarum Rhizoma中提取,对乙酰胆碱酯酶(AChE)有抑制作用,可用于治疗阿尔茨海默病。 |
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E4298 |
(-)-Carvone
|
(-)-Carvone是一种昆虫神经毒素,是乙酰胆碱酯酶 (AChE) 的不可逆抑制剂。 可用作驱鸟剂,抑制幼虫生长,降低化蛹率,增加幼虫死亡率。 |
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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。 |
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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. |
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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。 |
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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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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. |
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S5850 |
Vasicine
|
Vasicine,可分离自A. vasica,是一种生物碱。它是天然的cholinesterase(胆碱酯酶)抑制剂,在临床前模型中具有抗胆碱酯酶活性,可用于阿尔茨海默病的治疗药物开发。 |
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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. |
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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. |
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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. |
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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。 |
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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. |
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E0831 |
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。 |
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E2237 |
Vasicine (hydrochloride)
|
Vasicine hydrochloride(Peganine hydrochloride)是一种从Adhatoda vasica中分离出来的生物碱vasicine (VAS)的盐,是一种潜在的天然胆碱酯酶抑制剂。VAS抑制乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)。 |
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S3904 |
Isoimperatorin
|
Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. |
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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. |
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S4542 |
Trihexyphenidyl hydrochloride
|
Trihexyphenidyl hydrochloride (Benzhexol, Artane)是一种抗毒蕈碱类的抗帕金森病药物。 |
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S5511 |
Ethyl (triphenylphosphoranylidene) acetate
|
Ethyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
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S2082 |
Adiphenine HCl
|
Adiphenine HCl(NSC 129224) 是一种烟碱受体抑制剂,用作解痉药。 |
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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. |
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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。 |
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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 receptors和mAChRs。 |
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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。 |
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S9179 |
Catharanthine hemitartrate
|
Catharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
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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。 |
- bioRxiv, 2024, 2024.05.23.595327
- Biomedicines, 2022, 10(12)3056
- Elife, 2019, 8e45399
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S2508 |
Scopolamine (LSM-4015) HBr
|
Scopolamine HBr (LSM-4015,NSC 61806,(-)-Scopolamine hydrobromide, Hyoscine hydrobromide, Scopine hydrobromide)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。 |
- Heliyon, 2024, 10(1):e23945
- Zool Res, 2023, 44(4):712-724
- Zool Res, 2023, 44(4):712-724
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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
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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
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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。 |
- Neurosci Bull, 2023, none
- Neurochem Res, 2020, 10.1007/s11064-020-03103-1
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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。 |
- AAPS PharmSciTech, 2024, 25(7):204
- World J Gastroenterol, 2023, 29(20):3103-3118
- JCI Insight, 2017, 2(3):e89780
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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
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|
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。 |
- iScience, 2023, 26(3):106241
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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
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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
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S3117 |
Oxybutynin hydrochloride
|
Oxybutynin chloride(MJ4309-1)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
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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。 |
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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。 |
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S3048 |
Solifenacin succinate
|
Solifenacin succinate (YM905)是一种抗毒蕈碱类泌尿解痉药。 |
- J Immunother Cancer, 2024, 12(11)e009805
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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。 |
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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。 |
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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。 |
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S5480 |
Clidinium Bromide
|
Clidinium Bromide(Ro 2-3773) is an anticholinergic drug. |
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S6985 |
Varenicline
|
Varenicline(CP 526555)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。 |
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S4025 |
Homatropine Bromide
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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。 |
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S4027 |
Flavoxate HCl
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Flavoxate (NSC-114649)是一种毒蕈碱受体AChR拮抗剂, IC50为12.2 μM. |
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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
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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. |
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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. |
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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。 |
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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)。 |
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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。 |
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E3116 |
Acanthopanax Senticosus Extract
|
Acanthopanax Senticosus Extract提取自刺五加Acanthopanax Senticosus,对小鼠回肠功能具有通过毒蕈碱乙酰胆碱受体(mAChRs)收缩和直接弛缓的双重作用,其弛缓作用可用于治疗腹泻症状,使副交感神经活性增加。 |
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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。 |
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S9459 |
Mecamylamine Hydrochloride
|
Mecamylamine hydrochloride是一种口服活性、非选择性、非竞争性nAChR(烟碱型乙酰胆碱受体)拮抗剂。它也是一种神经节阻滞剂,可以穿过血脑屏障。 可用于神经精神疾病、高血压、抗抑郁领域的研究。 |
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E0829 |
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。 |
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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。 |
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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。 |
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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。 |
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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。 |
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S3735 |
Umeclidinium bromide
|
Umeclidinium bromide(GSK573719A)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。 |
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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
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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。 |
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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. |
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S6469 |
Thonzylamine
|
Thonzylamine (Neohetramine) 是抗组胺剂和抗胆碱能药。 |
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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 IκB 和 IKK 磷酸化来阻断 NF-κB 的活化。 |
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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。 |
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S4292 |
Diphenidol HCl
|
Diphenidol HCl(Diphenidol hydrochloride)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。
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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。 |
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S1913 |
Tropicamide
|
Tropicamide(Ro 1-7683)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。 |
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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。 |
- Viruses, 2024, 16(10)1559
- Heliyon, 2024, 10(1):e23945
- Theranostics, 2021, 11(12):5986-6005
|
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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。 |
- Front Neurosci, 2023, 17:1336026
- bioRxiv, 2023, 2023.11.10.566574
- Alzheimers Dement (N Y), 2022, 8(1):e12329
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S6887 |
CNO (Clozapine N-oxide)
|
CNO (Clozapine N-oxide)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。在溶液中不稳定,请现配现用! |
- Theranostics, 2024, 14(7):2881-2896
- Theranostics, 2024, 14(7):2881-2896
- Cell Rep, 2024, 43(8):114529
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S1805 |
Acetylcholine Chloride
|
化合物Acetylcholine Chloride(ACh 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)。 |
- Cell Mol Life Sci, 2024, 81(1):88
- iScience, 2023, 26(3):106241
- Cell, 2022, 185-21:3950-3965.e25
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S2455 |
Bethanechol chloride
|
Bethanechol chloride(Myocholine,Urecholine)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
|
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S2614 |
Arecoline HBr
|
Arecoline(NSC-31750)是一种毒蕈碱型乙酰胆碱受体激动剂。 |
- Antioxidants (Basel), 2024, 13(4)430
- Int J Oral Sci, 2024, 16(1):17
- Oncogene, 2020, 39(11):2437-2449
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S4171 |
Choline Chloride
|
Choline chloride(Hepacholine)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。 |
- Nat Commun, 2023, 14(1):5034
- Nat Commun, 2023, 14(1):5034
|
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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。 |
- Food Sci Nutr, 2022, 10(8):2773-2785
- Biotechnol Lett, 2020, 42(7):1219-1227
|
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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。 |
- Neuropharmacology, 2023, S0028-3908(23)00262-9
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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。 |
- Cell Rep Methods, 2023, 3(10):100599
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S4422 |
Nitenpyram
|
Nitenpyram(Bestguard,Capstar)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
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S2287 |
Cytisine
|
Cytisine (Baphitoxine, Sophorine)是一种烟碱型乙酰胆碱受体激动剂。 |
- Transl Oncol, 2023, 35:101712
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S6432 |
Cevimeline HCl hemihydrate
|
Cevimeline HCl hemihydrate(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。 |
- Front Pharmacol, 2022, 13:914153
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S0717 |
Varenicline (CP 526555) dihydrochloride
|
Varenicline (CP 526555) dihydrochloride 是 α4β2 nicotinic acetylcholine receptor (nAChR) 和 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。 |
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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。 |
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S0521 |
PNU-282987 S enantiomer free base
|
PNU-282987 S enantiomer free base是PNU-282987 free base的S-对映体,PNU-282987 free base是一种α7烟碱乙酰胆碱受体(α7 nicotinic acetylcholine receptor, α7 nAChR)激动剂。 |
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E0172 |
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。 |
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S5022 |
Varenicline Hydrochloride
|
Varenicline (CP 526555) Hydrochloride 是 α4β2 尼古丁乙酰胆碱受体 (nicotine acetylcholine receptor, nAChR) 和 α6β2 尼古丁乙酰胆碱受体 (nAChR) 的部分激动剂,Ki 值为 0.12 nM 和 0.14 大鼠纹状体中的 α6β2 nAChR 和 α4β2 nAChR 分别为 nM。 |
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E1876New |
GTS-21 dihydrochloride
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GTS-21 dihydrochloride(DMXB-A, DMBX-anabaseine)是 α7 烟碱型乙酰胆碱受体 (α7-nAChR) 的选择性激动剂,具有抗炎和认知增强活性。 GTS-21 diHClide 也是 α4β2 的拮抗剂,对人 α4β2 的 Ki 值为 20 nM,对 5-HT3A 受体 的 IC50 值为 3.1 μM。 |
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S7366 |
LY2119620
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LY2119620是一种人类M2 and M4 muscarinic acetylcholine receptors的特异变构激动剂。
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E0755 |
Guvacoline hydrochloride
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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。 |
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E4714New |
Xanomeline
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Xanomeline(LY-246708) 是毒蕈碱型 1(M(1) 受体 和 毒蕈碱型 4 受体(M(4) ) 的选择性激动剂。它能增加神经元兴奋性,抑制 D-苯丙胺和 (-)-阿扑吗啡诱发的行为。 |
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S4072 |
Decamethonium Bromide
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Decamethonium Bromide是一种烟碱AChR部分激动剂和神经肌肉阻断剂。 |
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S9789 |
JHU37152
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JHU37152 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq) 和 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。 |
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S9790 |
JHU37160
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JHU37160 是一种 Designer Receptors Exclusively Activated by Designer Drug (DREADD) 激动剂,对 human muscarinic acetylcholine M3 receptors (hM3Dq) 和 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。 |
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E1265 |
Deschloroclozapine
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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。 |
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S3684 |
Methacholine chloride
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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. |
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S5930 |
PNU 282987 HCl
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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。 |
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S4359 |
Carbamoylcholine chloride (Carbachol)
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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。此产品为危化品(急性毒性/易燃/皮肤腐蚀),请在穿戴防护面罩、防护手套和防护服后使用。 |
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S2957 |
Encenicline (EVP-6124) hydrochloride
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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。 |
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E0176 |
Dinotefuran
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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。 |
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S0457 |
DREADD agonist 21
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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。 |
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S6795 |
VU0357017 Hydrochloride
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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。 |
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