N-cyclohexylethyl-N-noroxymorphindole:: A μ-opioid preferring analogue of naltrindole

被引：9

作者：

Coop, A

Jacobson, AE

Aceto, MD

Harris, LS

Traynor, JR

Woods, JH

Rice, KC

机构：

[1] Univ Maryland, Sch Pharm, Dept Pharmaceut Sci, Baltimore, MD 21201 USA

[2] NIDDKD, Med Chem Lab, NIH, Bethesda, MD 20892 USA

[3] Virginia Commonwealth Univ, Med Coll Virginia, Dept Pharmacol, Richmond, VA 23298 USA

[4] Univ Michigan, Sch Med, Dept Pharmacol, Ann Arbor, MI 48109 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(00)00479-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The position of the indole in the indolomorphinans, which includes the delta opioid antagonist naltrindole, is considered to be responsible for the delta opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be mu preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2449 / 2451

页数：3

共 19 条

[1]

ABDELHAMID EE, 1991, J PHARMACOL EXP THER, V258, P299

[2] Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans [J].