Author/Authors :
Romano Di Fabio، نويسنده , , Maria Elvira Tranquillini، نويسنده , , Barbara Bertani، نويسنده , , Giuseppe Alvaro، نويسنده , , Fabrizio Micheli، نويسنده , , Fabio Sabbatini، نويسنده , , Maria Domenica Pizzi، نويسنده , , Giorgio Pentassuglia، نويسنده , , Alessandra Pasquarello، نويسنده , , Tommaso Messeri، نويسنده , , Daniele Donati، نويسنده , , Emiliangelo Ratti، نويسنده , , Roberto Arban، نويسنده , , Giovanna Dal Forno، نويسنده , , Angelo Reggiani، نويسنده , , Robert J. Barnaby، نويسنده ,
Abstract :
To identify neuroprotective agents after stroke, new substituted tetrahydroquinoline derivatives were designed as antagonists of the glycine binding site associated to the NMDA receptor, satisfying the key pharmacophoric requirements. In particular, the racemate 3c exhibited outstanding in vivo activity in the MCAo model in rats, when given iv both pre- and post-ischemia. Pure enantiomers 3c-(+) and 3c-(−) have been prepared following an original synthetic route. Despite the significant difference of activity observed in vitro, they shown similar neuroprotective profile in the MCAo model in rats.
