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Bioorg Med Chem Lett. 2009 Apr 15;19(8):2338-42. doi: 10.1016/j.bmcl.2009.02.056. Epub 2009 Feb 20.

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.

Author information

1
Neurosciences CEDD, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK. twatanabe@bikaken.or.jp

Abstract

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones have been identified as highly potent 5-HT(1A/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.

PMID:
19286377
DOI:
10.1016/j.bmcl.2009.02.056
[Indexed for MEDLINE]

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