5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinoli nones and 3,4-dihydro-2(1H)-quinolinones: Dual-acting 5-HT sub(1) receptor antagonists and serotonin reuptake inhibitors. Part 3

5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinoli nones and 3,4-dihydro-2(1H)-quinolinones: Dual-acting 5-HT sub(1) receptor antagonists and serotonin reuptake inhibitors. Part 3

5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinoli nones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT sub(1) autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The availability of tool compounds with a range of pr...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.7092-7096
Hauptverfasser: 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
Format: Artikel
Sprache:eng
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Animal models
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Zusammenfassung:5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinoli nones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT sub(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.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.09.085