Allosteric Modulation by Leucine-enkephalin of [3H]naloxone Binding in Rat Brain

Overview

Journal Eur J Pharmacol

Specialty Pharmacology

Date 1981 Jul 10

PMID 6268425

Citations 12

Authors

R B Rothman

T C Westfall

Affiliations

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Abstract

The interaction of morphine and leucine-enkephalin with the binding site labeled by [3H]naloxone in the presence of sodium was compared. The effect of fixed concentrations of morphine and leucine enkephalin on the saturation binding of [3H]naloxone demonstrated that whereas morphine was a competitive inhibitor, leucine enkephalin caused a dose-dependent masking of binding sites. From these data we conclude that the enkephalin receptor is allosterically coupled to the morphine receptor.

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