Invivo inactivation of γ-aminobutyric acid-α-ketoglutarate transaminase by 4-amino-5-fluoropentanoic acid

Richard B. Silverman*, Mark A. Levy, A. Jabbar Muztar, James D. Hirsch

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

Intraperitoneal injection into mice of varying concentrations of (S)-4-amino-5-fluoropentanoic acid ((S)-AFPA) produces a dose-dependent irreversible decrease in brain γ-aminobutyric acid-α-ketoglutaric acid aminotransferase (E.C. 2.6.1.19) activity. Concomitant with this inactivation is an increase in whole brain γ-aminobutyric acid (GABA) levels. Four hours after a dose of 100 mg/kg body weight of (S)-AFPA to mice, endogenous brain GABA concentrations increase to 16 times that of the untreated animals and the enzyme activity decreases to 20% that of the controls. The binding of (S)-AFPA to GABA receptors was more than three orders of magnitude poorer than for GABA itself.

Original languageEnglish (US)
Pages (from-to)520-523
Number of pages4
JournalBiochemical and Biophysical Research Communications
Volume102
Issue number1
DOIs
StatePublished - Sep 16 1981

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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