8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors—Part II

Steven M. Bromidge,Barbara Bertani,Manuela Borriello,Andrea Bozzoli,Stefania Faedo,Massimo Gianotti,Laurie J. Gordon,Matthew Hill,Valeria Zucchelli,Jeannette M. Watson,Laura Zonzini

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones have been identified as highly potent 5-HT1A/B/D receptor antagonists with and without additional SerT activity and a high degree of selectivity over hERG potassium channels. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization.

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关键词

5-HT1A/1B/1D antagonists,Serotonin reuptake inhibitors,5-HT1 autoreceptors,hERG,Antidepressant

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