Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging

  • ACS Med Chem Lett. 2016 Jan 20;7(3):245-9. doi: 10.1021/acsmedchemlett.5b00360.
Beilei Wang  1 ,  Zhenzhen Liu  1 ,  Zhao Ma  1 ,  Minyong Li  1 ,  Lupei Du  1
Affiliations
  • 1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
PMID: 26985309 DOI: 10.1021/acsmedchemlett.5b00360
Abstract

The detection and imaging of hERG potassium channels in living cells can provide useful information for hERG-correlation studies. Herein, three small-molecule fluorescent probes, based on the potent hERG channel inhibitor astemizole, for the imaging of hERG channels in hERG-transfected HEK293 cells (hERG-HEK293) and human colorectal Cancer cells (HT-29), are described. These probes are expected to be applied in the physiological and pathological studies of hERG channels.

Keywords
astemizole; cell imaging; fluorescent probes; hERG potassium channel.