Effect of γ-Aminobutyric Acid Derivatives, Especially, Homopantothenic Acid, on Excitability of the Brain

Abstract

Various derivatives of γ-aminobutyric acid (GABA) including homopantothenic acid (HOPA) were prepared and their seizureand excitation-suppressing action and sleep-prolonging effect were examined. The followings were observed: 1. A degree of suppressive effect against the usual convulsants was found with α-OH-GABA, N-carbobenzoxy-GABA and pantoyl derivatives and the effect was most pronounced with β-OH-GABA. 2. A delay in the appearance of the 2-methyl-4-amino-5-hydoxymethyl pyrimidine-induced running fit was noted with the amino-radical bound forms and especially, HOPA completely suppressed the seizure in a dose of 3mg/g. 3. The amino radical bound forms also inhibited the maximal seizure induced by electric shock and of these compounds, the pantoyl derivatives showed a trend for decline in the seizure threshold value. 4. The excitation enhanced by Philopon and Ritalin was suppressed by HOPA and pantothenic acid and especially in the former its effect was remarkable. 5. A prolongation of the duration of sleep produced by Auropan-Na was observed with the pantoyl derivatives, α-SH-GABA and N-carbobenzoxy-GABA.