Referenced in: none

Automatically associated channels: Kv11.1

Title: [3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel?

Authors: K Finlayson, A J Pennington, J S Kelly

Journal, date & volume: Eur. J. Pharmacol., 2001 Feb 2 , 412, 203-12

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/11166283

Abstract
The pharmacological characteristics of [3H]dofetilide binding in SHSY5Y, HEK293 and CHO-K1 cells were examined, and in parallel whole cell recordings used to characterise HERG-like K+ currents. Dofetilide affinity was similar in the human cell lines, SHSY5Y (Kd=99.6 nM) and HEK293 (Kd=102.9 nM), but 10 times lower in CHO-K1 cells (Kd=1200 nM). In contrast, clofilium and E4031 had a similar affinity in all three cell lines, whereas WAY 123,398 had no effect. Electrophysiological studies showed that SHSY5Y cells contained a HERG-like K+ current blocked by application of dofetilide to either side of the membrane. Block was faster when dofetilide was applied intracellularly. In contrast, HEK293 and CHO-K1 cells contained no such current, despite the presence of a partial cDNA for HERG in the former. That [3H]dofetilide is specific for I(Kr)/HERG may be questionable, as HEK293 and CHO-K1 cells contain no such functional K+ current.