GABAA receptor subtypes in sedation and hypnosis

Abstract

Drugs, such as sedative-hypnotics and anesthetics, are able to strongly regulate the vigilance state by affecting the main fast inhibitory neurotransmitter receptor system in the brain, the GABAA receptor system. Agonists, such as classical benzodiazepines, are today the most widely used hypnotics. This review summarizes the recent molecular and behavioral pharmacological advance to pinpoint the actions of various drugs on selected amino acid residues of the receptor subunits. As possible targets for future drug development, the properties of several GABAA receptor subtypes having critical localization in sleep-related brain nuclei/regions are reviewed on the basis of novel mouse models. It is predicted that the molecular heterogeneity of the GABAA receptor system holds promise for better and more selective drugs for sleep disorders.