The Neurochemical Mechanisms of the Pharmacological Activities of Inverse Agonists of the Benzodiazepine Binding Site

Abstract

Data on the basal (constitutive or spontaneous) activities of receptors, as well as their neurochemical and electrophysiological correlates, are presented. Inverse receptor agonists are a group of pharmacological drugs that can suppress constitutive activities. We describe the neurochemical mechanisms of the pharmacological activities of benzodiazepine binding site inverse agonists. These compounds inhibit chloride currents caused by gamma-aminobutyric acid at low non-physiological concentrations. This activity is the basis of the sobering action during the action of ethanol and the ability to suppress the addictive potential of psychoactive substances. In addition, the benzodiazepine binding site inverse agonists are able to activate memory formation processes and improve learning. The possible uses of drugs from this group in modern medicine are discussed. They may be used to treat a number of diseases in the fields of narcology, therapy, neurology, and psychiatry.