121667-28-5Relevant articles and documents
PRODRUGS OF GABA ANALOGS
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Paragraph 00221-00222, (2013/03/26)
The disclosures herein provide compounds of formula ?, formula II, formula 111 and formula IV or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, transmucosal, syrups, topical, extended or sustained release, or injection. Such compositions may be used to treatment of neurological disease and conditions such as neuropathic pain, diabetic neuropathic pain, epilepsy, restless leg syndrome, and other diseases related sub-chronic and chronic pain or its associated complications.
Synthesis and biological evaluation of GABA derivatives able to cross the blood-Brain barrier in rats
Carelli, Vincenzo,Liberatore, Felice,Scipione, Luigi,Giorgioni, Gianfabio,Di Stefano, Antonio,Impicciatore, Mariannina,Ballabeni, Vigilio,Calcina, Francesco,Magnanini, Francesca,Barocelli, Elisabetta
, p. 3765 - 3769 (2007/10/03)
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.
