6N-cinnamoyl-beta-naltrexamine and its p-nitro derivative. High efficacy kappa-opioid agonists with weak antagonist actions.

被引：10

作者：

Derrick, I

Moynihan, HA

Broadbear, J

Woods, JH

Lewis, JW

机构：

[1] UNIV BRISTOL,SCH CHEM,BRISTOL BS8 1TS,AVON,ENGLAND

[2] UNIV MICHIGAN,DEPT PHARMACOL,ANN ARBOR,MI 48109

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 02期

关键词：

D O I：

10.1016/0960-894X(95)00583-F

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

6N-cinnamoyl-beta-naltrexamine and its p-nitro derivative (7 and 8) are kappa-opioid agonists of high potency and exceptional efficacy and are only weakly effective mu opioid antagonists. This contrasts with the p-methyl analogue which has only low efficacy kappa-agonism but is a selective irreversible mu-antagonist like beta-FNA.

引用

页码：167 / 172

页数：6

共 7 条

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[2]

DERRICK L, IN PRESS J PHARM PHA

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