BIOLOGICAL ACTIONS In vivo AND In vitro OF TWO γ‐AMINOBUTYRIC ACID (GABA) ANALOGUES: β‐CHLORO GABA AND β‐PHENYL GABA
Open Access
- 1 November 1974
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 52 (3), 401-406
- https://doi.org/10.1111/j.1476-5381.1974.tb08609.x
Abstract
1 The synthesis of two analogues of γ-aminobutyric acid (GABA), β-chloro GABA and β-phenyl GABA is described. 2 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. 3 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. 4 Injection of β-phenyl GABA (200 mg/kg) into normal or epileptic cats (cobalt) caused the appearance of synchronized slow-wave EEG activity. 5 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. 6 β-Chloro GABA and β-phenyl GABA had no effect on the concentrations of catecholamines or of amino acids in mouse brain. 7 The results suggest that both β-chloro GABA and β-phenyl GABA may pass the blood-brain barrier.Keywords
This publication has 16 references indexed in Scilit:
- INHIBITION OF GABA TRANSAMINASE ACTIVITY BY 4‐AMINOTETROLIC ACIDJournal of Neurochemistry, 1972
- Motor phenomenology of cobalt experimental epileptic focus in the motor cortex of the cat during various stages of vigilanceElectroencephalography and Clinical Neurophysiology, 1972
- The action of a GABA derivative in human spasticityJournal of the Neurological Sciences, 1971
- A rapid, simplified procedure for simultaneous assay of norepinephrine, dopamine, and 5-hydroxytryptamine from discrete brain areasAnalytical Biochemistry, 1971
- The effect of aminooxyacetic acid on the metabolism of γ-aminobutyric acid in brainBiochemical Pharmacology, 1966
- THE EXCITATION AND DEPRESSION OF SPINAL NEURONES BY STRUCTURALLY RELATED AMINO ACIDSJournal of Neurochemistry, 1960
- Exchange reactions catalyzed by γ-aminobutyric-glutamic transaminaseBiochimica et Biophysica Acta, 1960
- ISOLATION OF FACTOR IJournal of Neurochemistry, 1957
- FACTOR I—INHIBITORY FACTOR FROM BRAINJournal of Neurochemistry, 1956
- The Determination of Enzyme Dissociation ConstantsJournal of the American Chemical Society, 1934