[Presynaptic component in the mechanism of fenibut action].
Superfusion of crude synaptosomal fractions from the rat brain cortex was used to study in vitro the effect of phenibut (beta-phenyl-GABA), a tranquilizing agent, on spontaneous and K+-stimulated release of 3H-GABA. It was found that phenibut in concentrations of 50 and 100 microM enhanced spontaneous tritium efflux by 15.9 and 30.7%, respectively. The effect of exogenous GABA in a concentration of 100 microM was 5 times more remarkable. The K+-stimulated release of the transmitter significantly increased under the effect of phenibut. Bicuculline counteracted this enhancement while picrotoxin did not effect the K+-stimulated egress of 3H-GABA. It is assumed that the presynaptic component described plays a role in the realization of the tranquilizing action of the tranquilizing action of phenibut.
D000818:Animals; D001418:Baclofen / Q000494:pharmacology; D001640:Bicuculline / Q000494:pharmacology; D002540:Cerebral Cortex / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D066298:In Vitro Techniques; D010852:Picrotoxin / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013574:Synaptosomes / Q000187:drug effects* / Q000502:physiology; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000502:physiology*
D001418:Baclofen; D001640:Bicuculline; D010852:Picrotoxin; D005680:gamma-Aminobutyric Acid; C008842:4-amino-3-phenylbutyric acid
Presinapticheskiĭ komponent v mekhanizme deĭstviia fenibuta.