Abstract
γ-Aminobutyric acid-α-ketoglutarate aminotransferase from rat and mouse brain was irreversibly inhibited by 5-fluoro-4-oxo-pentanoic acid, an analogue of succinic semi-aldehyde. The inhibition was concentration and temperature-dependent, and was initiated solely with the pyridoxamine form of the enzyme. All of the results to date are consistent with a catalytic mechanism for the inhibition. Intraperitoneal administration of 5-fluoro-4-oxo-pentanoic acid to rats or mice produced a dose-dependent, irreversible inhibition of brain γ-aminobutyric acid-α-ketoglutarate aminotransferase and elevation of brain GABA levels. No inhibition of glutamate decarboxylase, aspartate aminotransferase or alanine aminotransferase was observed.
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