Structure and Function of the Benzodiazepine Receptor

Abstract

Benzodiazepine tranquilizers are the most frequently therapeutically used psychotropic agents since their introduction in I960. Since 1974 research on the mechanism of action of agents acting on the specific benzodiazepine receptors (BZR) has been one of the hot areas of research in the neurosciences. – The BZR is an allosteric modulatory site on the GABAA-receptor-gated chloride channel through which γ-aminobutyric acid (GABA), the most important inhibitory neurotransmitter in the mammalian central nervous system, produces most of its effects. The uniqueness of the BZR is its ability to mediate two opposite effects (facilitating or depressing) on the GABAA-receptor function which can be blocked by specific antagonists. Research on the BZR has not only revealed the mechanism of action of an important class of tranquilizers and provided the basis for the development of novel innovative drugs, it has also led to a deep insight into the molecular and synaptic aspects of the central nervous system (CNS) functions.