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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

✍ Scribed by Steven M. Bromidge; Roberto Arban; Barbara Bertani; Manuela Borriello; Anna-Maria Capelli; Romano Di-Fabio; Stefania Faedo; Massimo Gianotti; Laurie J. Gordon; Enrica Granci; Alessandra Pasquarello; Simone K. Spada; Angela Worby; Laura Zonzini; Valeria Zucchelli


Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
642 KB
Volume
20
Category
Article
ISSN
0960-894X

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✦ Synopsis


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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