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April 16, 1982

Cellular Mechanisms of Benzodiazepine Action

Author Affiliations

From the Laboratory of Neurophysiology, National Institute of Neurological and Communicative Disorders and Stroke, National Institutes of Health, Bethesda, Md.

JAMA. 1982;247(15):2147-2151. doi:10.1001/jama.1982.03320400059039

BENZODIAZEPINES are in common clinical use because they possess a fortunate combination of important therapeutic properties. They are effective in the treatment of two common clinical conditions—anxiety and insomnia—and they are useful in the treatment of seizure disorders and certain kinds of spasticity as well. In addition to these therapeutic actions, these drugs lack significant side effects outside of the CNS and have low toxicity, factors that have contributed to their widespread clinical use. Since the introduction of chlordiazepoxide hydrochloride (Librium) in 1960, research into the cellular mechanisms of benzodiazepine action has increased in parallel with the use of these agents. In this review, some recent advances in elucidating the mechanisms of action of benzodiazepines in the CNS are described. The principal lines of basic research on benzodiazepines fall into two general categories: biochemical and electrophysiological. Although they will be discussed separately, they represent complementary strategies for achieving a comprehensive