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Molecular Pharmacology, Vol 6, 46-53, Copyright © 1970 by the American Society for Pharmacology and Experimental Therapeutics

Fluorinated ggr-Aminobutyric Acid

Enzymatic Synthesis and Biological Activity of a Potentially Useful Analogue

JAY C. UNKELESS 1 and PETER GOLDMAN 1

1 National Institute of Arthritis and Metabolic Diseases, National Institutes of Health, Bethesda, Maryland 20014

Glutamate decarboxylase (EC 4.1.1.15) of Escherichia coli reacts with L-ggr-fluoroglutamate to form agr-fluoro-ggr-aminobutyric acid. This reaction has been characterized, and the two fluorinated amino acids have been investigated as selective inhibitors of ggr-aminobutyric acid metabolism in the nervous system. L-ggr-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, agr-fluoro-ggr-aminobutyric acid inhibits the uptake of ggr-aminobutyric acid in a nerve-muscle preparatiom from lobster.

Submitted on September 24, 1969






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