Opiate Receptors: An Introduction

Abstract

Current status of opiate receptors and their agonists is reviewed — basic aspects of receptor theory, the importance of stereospecificity in drug-receptor interactions and the role of ‘second messengers’ in drug action. The three classes of endogenous opioids, originating from three distinct genes, are discussed: pro-opiomelanocortin, giving rise to β-endorphin, ACTH and various MSHs; pro-enkephalin, giving methionine enkephalin and leucine enkephalin; and prodynorphin; their anatomical distribution and the main classes of receptors with which they interact, the μ-receptor, with a high affinity for met-enkephalin and β-endorphin (as well as morphine and dynorphin A); the δ-receptor for which the primary ligand is leu-enkephalin; and the χ-receptor which is the main target for the dynorphins. Functional roles for endogenous opioids are considered. Essentially they are inhibitory to target neurones, depressing motor reflexes, baroreflexes and nociception. They also have roles in the response to physical and psychological stress.