奴芬克索(INN:nufenoxole;开发代号:SC-27166)是一种止泻药,作为外周选择性阿片受体激动剂,作用方式与洛哌丁胺类似。虽然它能够激活μ-阿片受体,但它无法穿过血脑屏障,因此具有选择性的抗腹泻作用,而不产生镇痛作用。[1][2][3][4][5]
事实速览 识别信息, CAS号 ...
奴芬克索![Thumb](//upload.wikimedia.org/wikipedia/commons/thumb/5/5e/Nufenoxole_Structure.svg/220px-Nufenoxole_Structure.svg.png) |
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2-[3-(2-azabicyclo[2.2.2]octan-2-yl)-1,1-diphenylpropyl]-5-methyl-1,3,4-oxadiazole
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CAS号 | 57726-65-5 |
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PubChem CID | |
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KEGG | |
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ChEMBL | |
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CompTox Dashboard (EPA) | |
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化学式 | C25H29N3O |
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摩尔质量 | 387.53 g·mol−1 |
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3D模型(JSmol) | |
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CC1=NN=C(O1)C(CCN2CC3CCC2CC3)(C4=CC=CC=C4)C5=CC=CC=C5
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InChI=1S/C25H29N3O/c1-19-26-27-24(29-19)25(21-8-4-2-5-9-21,22-10-6-3-7-11-22)16-17-28-18-20-12-14-23(28)15-13-20/h2-11,20,23H,12-18H2,1H3 Key:CVOCKGAVXLCEGM-UHFFFAOYSA-N
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关闭
US RE29556E,Adelstein GW,「1,1-Diaryl-1-oxadiazol-alkylamines」,发行于28 February 1978,指定于G.D. Searle & Company
Dajani EZ, Bianchi RG, East PF, Bloss JL, Adelstein GW, Yen CH. The pharmacology of SC-27166: a novel antidiarrheal agent. The Journal of Pharmacology and Experimental Therapeutics. December 1977, 203 (3): 512–26. PMID 411912.
Mackerer CR, Brougham LR, East PF, Bloss JL, Dajani EZ, Clay GA. Antidiarrheal and central nervous system activities of SC-27166 (2-[3 - 5 - methyl - 1, 3, 4 - oxadiazol - 2 - yl) - 3, 3 - diphenylpropyl] - 2 - azabicyclo [2.2.2]octane), a new antidiarrheal agent, resulting from binding to opiate receptor sites of brain and myenteric plexus. The Journal of Pharmacology and Experimental Therapeutics. December 1977, 203 (3): 527–38. PMID 200732.
Niemegeers CJ, McGuire JL, Heykants JJ, Janssen PA. Dissociation between opiate-like and antidiarrheal activities of antidiarrheal drugs. The Journal of Pharmacology and Experimental Therapeutics. September 1979, 210 (3): 327–33. PMID 480185.