Abstract
The main steps are presented that led to our current understanding of the interaction between benzodiazepine receptor ligands and the GABAA receptor. The benzodiazepine receptor is a modulatory site located on the GABAA receptor-chloride channel complex that has the unique property of being able to mediate positive as well as negative modulation of the chloride channel gating by the GABAA receptor. Some critical issues concerning the structure of the receptor-channel complex remain to be clarified. Research on the benzodiazepine-GABA interaction has led to novel concepts of drug action and receptor function and provides the basis for a whole spectrum of potential drugs with therapeutic utility.
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