Effect of Alkylpyrazine Derivatives on the Duration of Pentobarbital-Induced Sleep, Picrotoxicin-Induced Convulsion and γ-Aminobutyric Acid(GABA)Levels in the Mouse Brain

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The effect of alkylpyrazine derivatives on pentobarbital-induced sleeping time, picrotoxicin-induced convulsion and γ-aminobutyric acid(GABA)levels in mouse brain were studied. The duration of pentobarbital-induced sleep in mice was dose-dependently increased by 2, 5-dimethylpyrazine(DMP). The duration of pentobarbital-induced sleep was also increased by an administration route of intracerebroventricular injection. Sleep duration was also increased by the administration of isomers of DMP, 2-chloro-3, 6-dimethylpyrazine(DMP-Cl)and 2-fluoro-3, 6-dimethylpyrazine(DMP-F), but 3, 6-dimethylpyrazine-2-thiol(DMP-SH)did not affect sleep duration. The interval until the appearance of picrotoxicin-induced convulsion was prolonged by DMP and DMP-Cl. Increased sleep duration was obtained by administering DMP in combination with aminooxyacetic acid(AOAA)and diazepam compared to a single injection. The interval until convulsion due to picrotoxin was also prolonged by the administration of DMP combined with diazepam and valproic acid(VPA). The interval until the appearance of bicuculline-induced convulsion was also prolonged by pretreatment with DMP. The GABA level in mouse brain was increased by the administration of AOAA, VPA, DMP and DMP-Cl. These results suggest that DMP and other derivatives may strengthen the GABAnergic system in the brain.
公益社団法人日本薬学会の論文
2001-09-01