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103. GABA transaminase inhibitors.

Author

Ciesielski L, Simler S, Gensburger C, Mandel P, Taillandier G, Benoit-Guyod JL, Boucherle A, Cohen-Addad C, and Lajzerowicz J

Subjects
Aldehyde Oxidoreductases antagonists & inhibitors, Animals, Fatty Acids pharmacology, Kinetics, Mice, Molecular Conformation, Structure-Activity Relationship, Succinates, gamma-Aminobutyric Acid analogs & derivatives, 4-Aminobutyrate Transaminase antagonists & inhibitors, Transaminases antagonists & inhibitors
Abstract

In summary, several branched-chain fatty acids appeared to be competitive inhibitors of GABA-T and non-competitive inhibitors of SSADH. These compounds produce an increase in brain GABA level, and for two of these it was shown that the increase differs among various brain areas. An increase of GABA cannot be obtained by inhibition of SSADH. The increase in brain GABA seems to correlate with the anticonvulsant activity of branched-chain fatty acids.

Published
1979
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