Synthesis and biological evaluation of GABA derivatives able to cross the blood–Brain barrier in rats

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• 作者：Carelli ; Vincenzo ; Liberatore ; Felice ; Scipione ; Luigi ; Giorgioni ; Gianfabio ; Di Stefano ; Antonio ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2003
• 出版时间：November 3, 2003
• 年：2003
• 卷：13
• 期：21
• 页码：3765-3769
• 全文大小：168 K

文摘

Two new GABA derivatives, 1 and 2, were synthesized and tested for their capacity to display CNS activity, which was assessed by determining the effects on the duration of pentobarbital-induced hypnosis in rats. Compound 1, peripherally injected, significantly prolonged the hypnosis time, a typical GABA-mimetic effect, while both intracerebroventricular and intravenous administration of compound 2 surprisingly shortened the hypnotic effect in an atropine-sensitive way. The study was extended also to compounds 1a, 1b and 2a, putative oxidative/hydrolytic metabolites of 1 and 2.