Article date: November 1974
By: N.T. BUU, N.M. GELDER in Volume 52, Issue 3, pages 401-406
The synthesis of two analogues of γ‐aminobutyric acid (GABA), β‐chloro GABA and β‐phenyl GABA is described.
The activity of brain GABA aminotransferase was inhibited by β‐chloro GABA (5.7 × 10−5 M) and β‐phenyl GABA (4.6 × 10−3 M) in a competitive manner with GABA.
β‐Chloro GABA exhibited 50% of the inhibitory activity of GABA in blocking the discharge of the crayfish stretch receptor neurone; β‐phenyl GABA had no detectable effect.
Injection of β‐phenyl GABA (200 mg/kg) into normal or epileptic cats (cobalt) caused the appearance of synchronized slow‐wave EEG activity.
Administration of β‐chloro GABA (200 mg/kg) to epileptic cats (cobalt) produced a temporary diminution or abolition of epileptic discharges while causing no alteration in normal EEG activity.
β‐Chloro GABA and β‐phenyl GABA had no effect on the concentrations of catecholamines or of amino acids in mouse brain.
The results suggest that both β‐chloro GABA and β‐phenyl GABA may pass the blood‐brain barrier.
The synthesis of two analogues of γ‐aminobutyric acid (GABA), β‐chloro GABA and β‐phenyl GABA is described.
The activity of brain GABA aminotransferase was inhibited by β‐chloro GABA (5.7 × 10−5 M) and β‐phenyl GABA (4.6 × 10−3 M) in a competitive manner with GABA.
β‐Chloro GABA exhibited 50% of the inhibitory activity of GABA in blocking the discharge of the crayfish stretch receptor neurone; β‐phenyl GABA had no detectable effect.
Injection of β‐phenyl GABA (200 mg/kg) into normal or epileptic cats (cobalt) caused the appearance of synchronized slow‐wave EEG activity.
Administration of β‐chloro GABA (200 mg/kg) to epileptic cats (cobalt) produced a temporary diminution or abolition of epileptic discharges while causing no alteration in normal EEG activity.
β‐Chloro GABA and β‐phenyl GABA had no effect on the concentrations of catecholamines or of amino acids in mouse brain.
The results suggest that both β‐chloro GABA and β‐phenyl GABA may pass the blood‐brain barrier.
DOI: 10.1111/j.1476-5381.1974.tb08609.x
View this article