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N-Pivaloyl-leucyl-gamma-aminobutyric acid (PLG) is a synthetic dipeptide with a partition coefficient of 1.67 in an ethyl acetate/water system that partially inhibits the synaptosomal uptake and activates the release of [U-14C]gamma-aminobutyric acid [( U-14C]GABA). The displacement of GABA from crude synaptic membranes by PLG occurs with an IC50 of 10(-5) M. The compound has the capacity to cross the blood-brain barrier and increase central GABA levels. Its ED50 on cardiazol -induced convulsions is 60-65 mg/kg. PLG is resistant to hydrolysis by chymotrypsin and partially inhibits the proteolytic activity of trypsin.


L Galzigna, M Bianchi, A Bertazzon, A Barthez, G Quadro, M A Coletti-Previero. An N-protected gamma-aminobutyric acid dipeptide with anticonvulsant action. Journal of neurochemistry. 1984 Jun;42(6):1762-6

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PMID: 6547164

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