Guanidino N-substituted and N,N-disubstituted derivatives of the κ-opioid antagonist GNTI

被引：11

作者：

Black, SL

Chauvignac, C

Grundt, P

Miller, CN

Wood, S

Traynor, JR

Lewis, JW

Husbands, SM ^{[1
]}

机构：

[1] Univ Bath, Dept Pharm & Pharmacol, Bath BA2 7AY, Avon, England

[2] Univ Michigan, Dept Pharmacol, Ann Arbor, MI 48109 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 25期

关键词：

D O I：

10.1021/jm0309203

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Derivatives of the highly selective kappa-opioid receptor antagonist GNTI (2a) have been prepared. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells suggested that adding a benzyl or a substituted benzyl group to the guanidino moiety led, in general, to a retention of high kappa-affinity and antagonist potency. Disubstitution of the guanidino moiety led to reduced kappa-selectivity.

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页码：5505 / 5511

页数：7

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