Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives
4区 · 医学
Article
作者: Braje, Wilfried ; King, Linda L. ; Haupt, Andreas ; Delzer, Juergen ; Teschendorf, Hans-Juergen ; Hutchins, Charles W. ; Lubisch, Wilfried ; Steiner, Gerd ; Backfisch, Gisela ; Unger, Liliane ; Geneste, Herve ; Wernet, Wolfgang
The synthesis and SAR of novel and selective dopamine D(3)-receptor antagonists based on a 3,4-dihydro-1H-quinolin-2-one, a 1,3,4,5-tetrahydro-benzo[b]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzo[b]azepine-2,5-dione scaffold are discussed. A706149 (2.15mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigm.