Author/Authors :
Vincenzo Carelli، نويسنده , , Felice Liberatore، نويسنده , , Luigi Scipione، نويسنده , , Gianfabio Giorgioni، نويسنده , , Antonio Di Stefano، نويسنده , , Mariannina Impicciatore، نويسنده , , Vigilio Ballabeni، نويسنده , , Francesco Calcina، نويسنده , , Francesca Magnanini، نويسنده , , Elisabetta Barocelli، نويسنده ,
Abstract :
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.