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  • Title: Synthesis and biological evaluation of GABA derivatives able to cross the blood-brain barrier in rats.
    Author: Carelli V, Liberatore F, Scipione L, Giorgioni G, Di Stefano A, Impicciatore M, Ballabeni V, Calcina F, Magnanini F, Barocelli E.
    Journal: Bioorg Med Chem Lett; 2003 Nov 03; 13(21):3765-9. PubMed ID: 14552775.
    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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