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5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3 |
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| Authors: | Bromidge Steven M Arban Roberto Bertani Barbara Borriello Manuela Capelli Anna-Maria Di-Fabio Romano Faedo Stefania Gianotti Massimo Gordon Laurie J Granci Enrica Pasquarello Alessandra Spada Simone K Worby Angela Zonzini Laura Zucchelli Valeria |
| Affiliation: | Neurosciences CEDD, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK. steven.bromidge@evotec.com |
| Abstract: | 5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT(1) autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The availability of tool compounds with a range of profiles at targets known to play a key role in the control of synaptic 5-HT levels will allow exploration of different pharmacological profiles in a range of animal behavioral and disease models. |
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