14-desoxy analogues of naltrindole and 7-spiroindanyloxymorphone:: The role of the 14-hydroxy group at δ opioid receptors

被引：9

作者：

Kshirsagar, TA ^{[1
]}

Fang, XQ ^{[1
]}

Portoghese, PS ^{[1
]}

机构：

[1] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 41卷 / 14期

关键词：

D O I：

10.1021/jm980209b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：2657 / 2660

页数：4