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Pentobarbital: dual actions to increase brain benzodiazepine receptor affinity.

作者信息

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

出版信息

Science. 1981 Mar 27;211(4489):1448-50. doi: 10.1126/science.6258230.

DOI:10.1126/science.6258230
PMID:6258230
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 gamma-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 types of compounds.

摘要

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