Pentobarbital: dual actions to increase brain benzodiazepine receptor affinity.
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.[1]References
- Pentobarbital: dual actions to increase brain benzodiazepine receptor affinity. Skolnick, P., Moncada, V., Barker, J.L., Paul, S.M. Science (1981) [Pubmed]
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