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Bromidge SM, Bertani B, Borriello M, Faedo S, Gordon LJ, Granci E, Hill M, Marshall HR, Stasi LP, Zucchelli V, Merlo G, Vesentini A, Watson JM, Zonzini L: 6-[2-(4-Aryl-1-piperazinyl) ethyl]-2H-1,4-benzoxazin-3 (4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5653-6. Epub 2008 Aug 28.
Investigation of a series 6-[2-(4-aryl-1-piperazinyl) ethyl]-2H-1,4-benzoxazin-3 (4H)-ones has led to the discovery of potent 5-HT (1A/1B/1D) receptor antagonists with and without additional SerT affinity. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization. |
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