TY - JOUR T1 - Fluorinated γ-Aminobutyric Acid JF - Molecular Pharmacology JO - Mol Pharmacol SP - 46 LP - 53 VL - 6 IS - 1 AU - JAY C. UNKELESS AU - PETER GOLDMAN Y1 - 1970/01/01 UR - http://molpharm.aspetjournals.org/content/6/1/46.abstract N2 - Glutamate decarboxylase (EC 4.1.1.15) of Escherichia coli reacts with L-γ-fluoroglutamate to form α-fluoro-γ-aminobutyric acid. This reaction has been characterized, and the two fluorinated amino acids have been investigated as selective inhibitors of γ-aminobutyric acid metabolism in the nervous system. L-γ-Fluoroglutamate inhibits the glutamate decarboxylase from calf brain (Ki = 1.4 x 10-2 M) at concentrations comparable to the Km of this enzyme for glutamate (10-2 M). In addition, α-fluoro-γ-aminobutyric acid inhibits the uptake of γ-aminobutyric acid in a nerve-muscle preparatiom from lobster. ER -