[Presynaptic component in the mechanism of fenibut action]

Biull Eksp Biol Med. 1982 Nov;94(11):59-61.
[Article in Russian]


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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Baclofen / pharmacology
  • Bicuculline / pharmacology
  • Cerebral Cortex / physiology
  • Dose-Response Relationship, Drug
  • In Vitro Techniques
  • Picrotoxin / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Synaptosomes / drug effects*
  • Synaptosomes / physiology
  • gamma-Aminobutyric Acid / analogs & derivatives*
  • gamma-Aminobutyric Acid / pharmacology
  • gamma-Aminobutyric Acid / physiology*


  • Picrotoxin
  • gamma-Aminobutyric Acid
  • Baclofen
  • 4-amino-3-phenylbutyric acid
  • Bicuculline