奴芬克索

奴芬克索
识别信息
  • 2-[3-(2-azabicyclo[2.2.2]octan-2-yl)-1,1-diphenylpropyl]-5-methyl-1,3,4-oxadiazole
CAS号57726-65-5
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
化学信息
化学式C25H29N3O
摩尔质量387.53 g·mol−1
3D模型（JSmol（英语：JSmol））
  • CC1=NN=C(O1)C(CCN2CC3CCC2CC3)(C4=CC=CC=C4)C5=CC=CC=C5
  • 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

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]

参见

参考资料

  1. ^ US RE29556E,Adelstein GW,「1,1-Diaryl-1-oxadiazol-alkylamines」,发行于28 February 1978,指定于G.D. Searle & Company 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ Korey A, Zilm DH, Sellers EM. Dependence liability of two antidiarrheals, nufenoxole and loperamide. Clinical Pharmacology and Therapeutics. May 1980, 27 (5): 659–64. PMID 7371363. S2CID 35222789. doi:10.1038/clpt.1980.93.