Kovalev G I, Prikhozhan A V, Raevskiĭ K S
Biull Eksp Biol Med. 1982 Nov;94(11):59-61.
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.
利用大鼠大脑皮层粗制突触体组分的灌注法，在体外研究了镇定剂苯乙胺（β-苯基-GABA）对3H-GABA自发释放和钾离子刺激释放的影响。发现浓度为50和100微摩尔的苯乙胺分别使自发氚外流增加了15.9%和30.7%。浓度为100微摩尔的外源性GABA的作用则显著5倍。在苯乙胺的作用下，递质的钾离子刺激释放显著增加。荷包牡丹碱可抵消这种增强作用，而印防己毒素对3H-GABA的钾离子刺激外流没有影响。据推测，所述的突触前成分在苯乙胺镇定作用的实现中起作用。
