[Is the benzodiazepine binding site a receptor?]

Abstract

The benzodiazepines bind to high affinity sites on neuronal membranes in the central nervous system. These sites form part of a multimolecular postsynaptic complex which also includes the GABA receptor and its ionophore. The benzodiazepine binding sites appear to present a certain heterogeneity which may correspond to a diversity of functions. A good correlation exists between the pharmacological potencies of the various benzodiazepines and their affinities for the receptor in vitro, but the relationship is less clear when binding is studied in vivo. Nevertheless, high affinity benzodiazepine binding remains an essential tool for the pharmacologist in search of more specific drugs.