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The in vivo inhibition of gaba-transaminase by gabaculine

1977; Elsevier BV; Volume: 76; Issue: 4 Linguagem: Inglês

10.1016/0006-291x(77)90993-7

1090-2104

Robert R. Rando, Faan Wen Bangerter,

Bioactive natural compounds

The naturally occurring amino acid gabaculine ((−)-5-amino-1,3 cyclohexadiene carboxylic acid) is a potent irreversible inhibitor of mouse brain γ-aminobutyric acid (GABA)-α-ketoglutaric acid transaminase. When administered I.P. gabaculine, irreversibly inhibits the mouse brain enzyme in a time dependent fashion. Concomitant with this inhibition is a rise in endogenous brain GABA levels. Administration of gabaculine at a concentration of 100 mg/kg mouse leads to the complete inhibition of the enzyme after 4 hrs. Brain levels of GABA continually rise after the administration of the drug. After 20 hrs they are 15–20 times higher than levels in the untreated animals.