GABA receptors and benzodiazepines.

From an historical standpoint, the development of our understanding of basic mechanisms of the actions of gamma aminobutyric acid (GABA) and benzodiazepines began on separate paths. Classical pharmacology revealed similarity between the actions of GABA and benzodiazepines in the central nervous system. Furthermore, pharmacological experiments with selective agonists and antagonists indicated that there exists subtypes of both GABA and benzodiazepine receptors and that the actions of the benzodiazepines are produced by modulation of GABA effects. Thus the two paths of research on GABA and benzodiazepines had crossed in explaining the effects of benzodiazepines by an interaction with GABAA receptors that were located on the same macromolecular complex. More recently, this interaction has been elucidated further by the cloning of subunits of GABAA receptors: the interaction between GABA and benzodiazepines is now being explained at a molecular level.