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BIOLOGICAL ACTIONS In vivo AND In vitro OF TWO γ‐AMINOBUTYRIC ACID (GABA) ANALOGUES: β‐CHLORO GABA AND β‐PHENYL GABA
Author(s) -
BUU N.T.,
GELDER N.M.
Publication year - 1974
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1974.tb08609.x
Subject(s) - gamma aminobutyric acid , gabaa receptor , beta (programming language) , inhibitory postsynaptic potential , in vivo , chemistry , aminobutyric acid , cats , bicuculline , neurotransmission , medicine , endocrinology , pharmacology , receptor , biochemistry , biology , microbiology and biotechnology , computer science , programming language
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.