173252-60-3Relevant academic research and scientific papers
8-Methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines : Highly potent in vivo AMPA antagonists
Mignani, Serge,Bohme, Georg Andrees,Boireau, Alain,Cheve, Michel,Damour, Dominique,Debono, Marc-Williams,Genevois-Borella, Arielle,Imperato, Assunta,Jimonet, Patrick,Pratt, Jeremy,Randle, John C.R.,Ribeill, Yves,Vuilhorgne, Marc,Stutzmann, Jean-Marie
, p. 591 - 596 (2000)
A novel series of readily water soluble 8-methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines were synthesized. The -10-yl acetic acid ((+)-3) and -10-carboxylidene (4) derivatives exhibit potent affinities (IC50 = 4 and 19 nM, respectively) and antagonist properties (IC50 = 2 and 3 nM, respectively) at the ionotropic AMPA receptor. These compounds also display anticonvulsant properties against both electrically and sound-induced convulsions in mice after ip, sc and iv administration with ED50 values between 0.9 and 11 mg/kg, thus suggesting adequate brain penetration. (C) 2000 Elsevier Science Ltd. All rights reserved.
