Abstract
ABSTRACT The discovery of benzodiazepine receptors in 1977 signalled a new era in understanding of the mechanism of action of benzodiazepines. The receptors were found to be located on brain neurons and to be highly specific for clinically and pharmacologically active benzodiazepines. Benzodiazepine receptors appear to be the physiological target for the action of benzodiazepines. It was anticipated that benzodiazepine receptors, like many other receptors such as β–receptors, dopamine receptors, etc., might be labile structures which could be modulated by agents and changes in the micro – and macroenvironment. This report shortly reviews and slightly extends studies on benzodiazepine receptor modulation. It appeared to be rather difficult to modulate benzodiazepine receptors in living rats by chronic benzodiazepine treatment or by prolonged exposure to stress (foot – shock, cold water swimming, etc.). On the other hand, several types of seizures slightly increase or otherwise affects benzodiazepine receptors. Several of these ex vivo studies on benzodiazepine receptor modulation, however, need reinvestigation in view of recent developments in understanding of GABA/benzodiazepine receptor interactions and receptor heterogeneity.
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