OPIOID ACTIVITIES OF FRAGMENTS OF BETA-ENDORPHIN AND OF ITS LEUCINE-65-ANALOG - COMPARISON OF THE BINDING-PROPERTIES OF METHIONINE-ENKEPHALIN AND LEUCINE-ENKEPHALIN

被引：110

作者：

WATERFIELD, AA ^{[1
]}

LESLIE, FM ^{[1
]}

LORD, JAH ^{[1
]}

LING, N ^{[1
]}

KOSTERLITZ, HW ^{[1
]}

机构：

[1] SALK INST BIOL STUDIES, NEUROENDOCRINOL LABS, LA JOLLA, CA 92037 USA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1979年 / 58卷 / 01期

关键词：

Leu[!sup]65[!/sup]-analogue fragments; [!sup]3[!/sup]H]-Leucin-enkephalin binding; [!sup]3[!/sup]H]-Methione-enkephalin binding; β-Endorphin fragments; δ-Receptors; μ-Receptors;

D O I：

10.1016/0014-2999(79)90334-0

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

For characterisation in vitro, four parallel assays were used: the guinea pig ileum and mouse vas deference as pharmacological models at 36°C and the inhibition of binding of [3H]-leucine-enkephalin and [3H]-methionine-enkephalin at 0°C. The Leu65-analogue of β-endorphin and its pragments (61-65, 61-76 and 61-77) have a lower affinity to the [3H]-naltrexone binding site or μ-receptors than the corresponding Met65-peptides whereas no such difference was found for the [3H]leucine-enkephalin binding sites or δ-receptors. When the binding of [3H]-methionine-enkephalin or [3H]-leucine-enkephalin was inhibited by cold ligands interacting with δ-, μ-, or κ-receptors, no evidence was obtained for more than one type of δ-binding site. © 1979.

引用

页码：11 / 18

页数：8

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