纳曲吲哚和7-螺茚满氧基吗啡的14-去氧类似物：δ阿片受体上14-羟基的作用

14-Desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: the role of the 14-hydroxy group at delta opioid receptors.

作者信息

Kshirsagar T A, Fang X, Portoghese P S

机构信息

Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, USA.

出版信息

J Med Chem. 1998 Jul 2;41(14):2657-60. doi: 10.1021/jm980209b.

DOI:10.1021/jm980209b

Abstract

The 14-hydroxy group is known to increase the antagonist potency of mu-selective opioid ligands. To investigate the role of this group at the delta opioid receptor, the 14-desoxy analogues (7 and 9) of the delta-selective ligands, naltrindole (1, NTI) and spiroindanyloxymorphone (2, SIOM), have been synthesized and tested. The in vitro pharmacologic activities of 7 and 9 suggest that the 14-hydroxy group plays an important role in determining the delta selectivity and potency of NTI and SIOM.

摘要

已知14-羟基可增强μ-选择性阿片样物质配体的拮抗效力。为研究该基团在δ阿片受体上的作用，已合成并测试了δ-选择性配体纳曲吲哚（1，NTI）和螺环茚满氧基吗啡（2，SIOM）的14-脱氧类似物（7和9）。7和9的体外药理活性表明，14-羟基在决定NTI和SIOM的δ选择性和效力方面起着重要作用。

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