GABA(A)-RECEPTOR SUBTYPES - CLINICAL EFFICACY AND SELECTIVITY OF BENZODIAZEPINE SITE LIGANDS

The main inhibitory neurotransmitter receptor of the brain, the gamma- aminobutyric acid type A receptor (GABA(A)), mediates the actions of s everal classes of clinically important drugs, such as benzodiazepines, barbiturates and general anaesthetics. This review summarizes the cur rent knowledge on how classical benzodiazepines and novel nonbenzodiaz epine compounds act on the benzodiazepine site of GABA, receptors and on their clinical pharmacology related to anxiolytic, sedative, hypnot ic and cognitive effects or side-effects. Partial agonism, receptor su btype selectivity and novel binding sites are discussed as possible st rategies to develop new drugs with fewer adverse effects than are seen in the clinical use of benzodiazepines.