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An N‐Protected γ‐Aminobutyric Acid Dipeptide with Anticonvulsant Action
Author(s) -
Galzigna L.,
Bianchi M.,
Bertazzon A.,
Barthez A.,
Quadro G.,
ColettiPreviero M. A.
Publication year - 1984
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1984.tb12769.x
Subject(s) - chemistry , dipeptide , anticonvulsant , aminobutyric acid , chymotrypsin , inhibitory postsynaptic potential , ed50 , gamma aminobutyric acid , trypsin , biochemistry , stereochemistry , pharmacology , amino acid , enzyme , in vitro , neuroscience , biology , receptor , epilepsy
N ‐Pivaloyl‐leucyl–γ‐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‐ 14 C]‐γ‐aminobutyric acid ([U‐ 14 C]GABA). The displacement of GAB A from crude synaptic membranes by PLG occurs with an IC 50 of 10 −5 M . The compound has the capacity to cross the blood‐brain barrier and increase central GABA levels. Its ED 50 on cardiazol‐induced convulsions is 60‐65 mg/kg. PLG is resistant to hydrolysis by chymotrypsin and partially inhibits the proteolytic activity of trypsin.