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.
D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects; D002712:Chlorides / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism; D008297:Male; D010424:Pentobarbital / Q000494:pharmacology*; D051381:Rats; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism; D011963:Receptors, GABA-A; D013268:Stimulation, Chemical; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D002712:Chlorides; D011955:Receptors, Drug; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid; D010424:Pentobarbital; D003975:Diazepam