| Abstract: | In this short review, evidence is presented to show that the benzodiazepines produce their variety of pharmacological effects by activating specific receptors that form part of the main inhibitory neurotransmitter receptor system, the γ‐amino‐butyric acid (GABA) system, in the mammalian brain. Different classes of benzodiazepine receptor ligands have been developed which can alleviate anxiety or produce anxiety according to the fine structural changes that occur when the ligands interact with the benzodiazepine receptor. There is some evidence that endogenous substances in the brain can cause either an increase or a reduction in the anxiety state by acting on the benzodiazepine receptor. The unique nature of the benzodiazepine receptor, and the disparate properties of the drugs that act on this receptor, should allow plenty of scope for the development of novel compounds with selective anxiolytic and other properties in the future. Lastly, despite the evidence from animal studies that benzodiazepine receptor function changes in response to drug treatment, there is little evidence from human brain studies that such changes are relevant to the phenomena of tolerance, dependence and withdrawal effects that have been the recent cause for public concern. Copyright © 1999 John Wiley & Sons, Ltd. |
