Benzodiazepine Receptor-Mediated “Anxiety” in Primates
During the past seven years, numerous investigations have demonstrated that the benzodiazepine receptor [in concert with an associated recognition site for GABA and a chloride ionophore] is involved in the antianxiety (anxiolytic) actions of a number of chemically unrelated substances such as the benzodiazepines, barbiturates, triazolopyridazines (e.g. CL 218,872), pyrazolopyridines (e.g. SQ 65,396), and ethanol (Skolnick and Paul, 1981). During the past three years, several compounds have been described which bind to benzodiazepine receptors with high affinities, and antagonize one or more of the pharmacologic actions of the benzodiazepines (Skolnick et al., 1982). The first of these benzodiazepine antagonists described was the ethyl ester of beta carboline-3-carboxylic acid (Tenen and Hirsch, 1980; Oakley and Jones, 1980). Although this compound was first postulated to be an endogenous ligand of the benzodiazepine receptor (Braestrup, et al., 1980), it is likely that this compound as well as the related beta carbolines extracted from human urine were formed during the isolation procedure employed (Squires, 1981). Nonetheless, these compounds have proven invaluable in both better defining the physiologic role(s) of the benzodiazepine receptor complex and providing a robust, chemically induced model of anxiety in primates.
KeywordsEthyl Ester Acid Ethyl Ester Intrinsic Action Beta Endorphin Convulsant Action
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