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Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com |
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| Authors: | Geneste Hervé Backfisch Gisela Braje Wilfried Delzer Jürgen Haupt Andreas Hutchins Charles W King Linda L Lubisch Wilfried Steiner Gerd Teschendorf Hans-Jürgen Unger Liliane Wernet Wolfgang |
| Institution: | Abbott GmbH & Co. KG, Discovery Research, D-67008 Ludwigshafen, Germany. |
| Abstract: | 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-benzob]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzob]azepine-2,5-dione scaffold are discussed. A706149 (2.15mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigm. |
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