Referenced in: none

Automatically associated channels: Kv11.1

Title: 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.

Authors: 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

Journal, date & volume: Bioorg. Med. Chem. Lett., 2009 Apr 15 , 19, 2338-42

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/19286377

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.