Opioid κ Receptors as a Molecular Target for the Creation of a New Generation of Analgesic Drugs

Abstract

This review provides a brief description of the main structural and functional features of the κ opioid receptor, along with the properties of its agonists and the potential for using these in medicine. Of all the opioid receptor subtypes, κ receptors are the most attractive in terms of creating new drugs with a minimum of side effects. The opioid κ receptor is a member of the superfamily of metabotropic G-protein-coupled receptors. Opioid κ receptors are widely distributed in the CNS and at the periphery. They are involved in numerous physiological processes, including analgesia, regulation of neuroendocrine secretion, water balance, drinking and feeding behavior, autonomic functions, and the mechanisms of learning and memory. Data have been reported on the existence of three subtypes of κopioid receptor, though the molecular properties of only subtype 1 (ê₁) have been studied.