Spiro-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives are mixed AMPA and NMDA glycine-site antagonists active in vivo |
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| Authors: | Jimonet P Boireau A Chevé M Damour D Genevois-Borella A Imperato A Pratt J Randle J C Ribeill Y Stutzmann J M Mignani S |
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| Affiliation: | Rh?ne-Poulenc S.A., Rh?ne-Poulenc Rorer, Centre de Recherche de Vitry-Alfortville, Vitry-sur-Seine, France. |
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| 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 (+)-3e was notably more potent than the levorotatory isomer (-)-3e in in vitro and in vivo assays. |
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