Synthesis and biological evaluation of GABA derivatives able to cross the blood-brain barrier in rats |
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| Authors: | Carelli Vincenzo Liberatore Felice Scipione Luigi Giorgioni Gianfabio Di Stefano Antonio Impicciatore Mariannina Ballabeni Vigilio Calcina Francesco Magnanini Francesca Barocelli Elisabetta |
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| Institution: | Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, Piazzale A. Moro 5, 00185 Rome, Italy. vincenzo.carelli@uniroma1.it |
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| 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. |
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