Pentobarbital: Dual actions to increase brain benzodiazepine receptor affinity

P. Skolnick, V. Moncada, J. L. Barker, S. M. Paul

Research output: Contribution to journalArticlepeer-review

95 Scopus citations

Abstract

The binding of [3H]diazepam to benzodiazepine receptors was studied in extensively washed membranes of rat cerebral cortex in the presence of the depressant barbiturate, pentobarbital. Pentobarbital, like the endogenous neurotransmitter γ-aminobutyric acid (GABA), increased the basal binding and also potentiated the GABA-enhanced binding of [3H]diazepam to benzodiazepine receptors by increasing the apparent affinity of [ 3H]diazepam for the benzodiazepine receptor. The concentrations of pentobarbital necessary to elicit these effects in vitro are the same as those observed after treatment with pharmacologically relevant doses, suggesting that a common neurochemical association may exist between these two types of compounds.

Original languageEnglish
Pages (from-to)1448-1450
Number of pages3
JournalScience
Volume212
Issue number4489
StatePublished - Jan 1 1981

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