THE SELECTIVITY OF THE OPIOID ANTAGONIST, NALTRINDOLE, FOR DELTA-OPIOID RECEPTORS

被引：51

作者：

ROGERS, H ^{[1
]}

HAYES, AG ^{[1
]}

BIRCH, PJ ^{[1
]}

TRAYNOR, JR ^{[1
]}

LAWRENCE, AJ ^{[1
]}

机构：

[1] LOUGHBOROUGH UNIV TECHNOL,DEPT CHEM,LOUGHBOROUGH LE11 3TU,LEICS,ENGLAND

来源：

JOURNAL OF PHARMACY AND PHARMACOLOGY | 1990年 / 42卷 / 05期

关键词：

D O I：

10.1111/j.2042-7158.1990.tb05428.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Abstract— In the mouse vas deferens, naltrindole gave pKB values of 9.7, 8.3, and 7.5 at the δ‐, μ‐, and K‐sites and in binding assays, pIC50 values of 9.6, 7.8 and 7.2 at the same sites. The affinity of naltrindole for the δ binding site was increased in the presence of sodium ions and 5′‐guanylylimidophosphate. Naltrindole is, thus, a potent opioid antagonist with marked selectivity for the δ‐opioid receptor. 1990 Royal Pharmaceutical Society of Great Britain

引用

页码：358 / 359

页数：2

共 8 条

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