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Science 27 March 1981:
Vol. 211. no. 4489, pp. 1448 - 1450
DOI: 10.1126/science.6258230
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Articles

Science, Vol 211, Issue 4489, 1448-1450
Copyright © 1981 by American Association for the Advancement of Science

articles

Pentobarbital: dual actions to increase brain benzodiazepine receptor affinity

P Skolnick, V Moncada, JL Barker, and SM Paul

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.


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Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor.
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Numbers of receptor sites from Scatchard graphs: facts and fantasies.
I. Klotz (1982)
Science 217, 1247-1249
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