Title of article :
Spiro-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives are mixed AMPA and NMDA glycine-site antagonists active in vivo
Author/Authors :
Patrick Jimonet، نويسنده , , Alain Boireau، نويسنده , , Michel Chevé، نويسنده , , Dominique Damour، نويسنده , , Arielle Genevois-Borella، نويسنده , , Assunta Imperato، نويسنده , , Jeremy Pratt، نويسنده , , John C.R. Randle، نويسنده , , Yves Ribeill، نويسنده , , Jean-Marie Stutzmann، نويسنده , , Serge Mignani، نويسنده ,
Abstract :
Original spiro-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives were synthesised and led to the identification of 3e which showed good affinities for both the AMPA and the NMDA glycine-site receptors, and displayed good anticonvulsant effects after i.p. and i.v. administrations in the electroshock-induced convulsion assay in mice. The corresponding dextrorotatory isomer (+)-3d was notably more potent than the levorotatory isomer (−)-3e in in vitro and in vivo assays.
