2. Academic Validation
  3. 4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with in vivo activity

4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with in vivo activity

  • Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7. doi: 10.1016/s0960-894x(00)00181-5.
J M Stutzmann 1,  G A Bohme,  A Boireau,  D Damour,  M W Debono,  A Genevois-Borella,  A Imperato,  P Jimonet,  J Pratt,  J C Randle,  Y Ribeill,  M Vuilhorgne,  S Mignani
Affiliations

Affiliation

  • 1 Aventis Pharma S.A., Centre de Recherche de Vitry-Alfortville, Vitry-sur-Seine, France.
PMID: 10843235 DOI: 10.1016/s0960-894x(00)00181-5
Abstract

A novel series of 2-substituted-4,5-dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazine derivatives was synthesised. One of them, 4e-a highly water soluble compound exhibited a nanomolar affinity and demonstrated competitive antagonist properties at the ionotropic AMPA receptors. This compound also displayed potent anticonvulsant properties against electrically or sound-induced convulsions in mice after systemic administration, thus suggesting adequate brain penetration.

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