RT Journal Article
SR Electronic
T1 Fluorinated γ-Aminobutyric Acid
JF Molecular Pharmacology
JO Mol Pharmacol
FD American Society for Pharmacology and Experimental Therapeutics
SP 46
OP 53
VO 6
IS 1
A1 JAY C. UNKELESS
A1 PETER GOLDMAN
YR 1970
UL http://molpharm.aspetjournals.org/content/6/1/46.abstract
AB 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.