OPIATE RECEPTOR-BINDING AFFECTED DIFFERENTIALLY BY OPIATES AND OPIOID PEPTIDES

被引：190

作者：

CHILDERS, SR

CREESE, I

SNOWMAN, AM

SNYDER, SH

机构：

[1] JOHNS HOPKINS UNIV,SCH MED,DEPT PHARMACOL,BALTIMORE,MD 21205

[2] JOHNS HOPKINS UNIV,SCH MED,DEPT EXPTL THERAPEUT,BALTIMORE,MD 21205

[3] JOHNS HOPKINS UNIV,SCH MED,DEPT PSYCHIAT,BALTIMORE,MD 21205

[4] JOHNS HOPKINS UNIV,SCH MED,DEPT BEHAV SCI,BALTIMORE,MD 21205

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1979年 / 55卷 / 01期

关键词：

Opiate receptors; Opiates; Opioid peptides;

D O I：

10.1016/0014-2999(79)90142-0

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The potencies of various opiates in displacing several 3H-opiates ligands′ binding to rat brain membranes vary depending on the nature of the ligand. Whereas opiate antagonists, as well as the opioid peptides and somes agonists (etorphine, levorphanol and phenazocine) display similar affinities in displacing either 3H-opiate or 3H-methionine enkephalin binding, other agonists (such as morphine and oxymorphone) are considerably (20-50 times) weaker in displacing 3H-enkephalin than 3H-dihydromorphine binding. These agonists also compete for 3H-enkephalin binding with shallow displacement curves, and are greatly weakened in displacing 3H-naloxone binding in the presence of sodium. These agonists differ from the other opiate classes by processing a relatively hydrophilic component in their C-ring moieties which may provide a basis for the differential interactions of drugs with the opiate receptor. © 1979.

引用

页码：11 / 18

页数：8

共 31 条

[11] ENERGY CONFORMATION STUDY OF MET-ENKEPHALIN AND ITS D-ALA2 ANALOG AND THEIR RESEMBLANCE TO RIGID OPIATES [J].