Document Detail

[3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel?
MedLine Citation:
PMID:  11166283     Owner:  NLM     Status:  MEDLINE    
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.
K Finlayson; A J Pennington; J S Kelly
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  412     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  2001 Feb 
Date Detail:
Created Date:  2001-02-22     Completed Date:  2001-05-10     Revised Date:  2008-10-28    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  203-12     Citation Subset:  IM    
Fujisawa Institute of Neuroscience, Department of Neuroscience, University of Edinburgh, 1 George Square, EH8 9JZ, Edinburgh, UK.
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MeSH Terms
Anti-Arrhythmia Agents / metabolism*,  pharmacology
Benzimidazoles / pharmacology
Binding Sites
Cation Transport Proteins*
Cell Line
DNA-Binding Proteins*
Dose-Response Relationship, Drug
Ether-A-Go-Go Potassium Channels
Membrane Potentials / drug effects
Patch-Clamp Techniques
Phenethylamines / metabolism*,  pharmacology
Potassium Channel Blockers
Potassium Channels / metabolism*
Potassium Channels, Voltage-Gated*
Protein Binding
Quaternary Ammonium Compounds / pharmacology
RNA / metabolism
Radioligand Assay
Sulfanilamides / pharmacology
Sulfonamides / metabolism*,  pharmacology
Tumor Cells, Cultured
Reg. No./Substance:
0/Anti-Arrhythmia Agents; 0/Benzimidazoles; 0/Cation Transport Proteins; 0/DNA-Binding Proteins; 0/ERG protein, human; 0/ERG1 potassium channel; 0/Ether-A-Go-Go Potassium Channels; 0/KCNH6 protein, human; 0/Phenethylamines; 0/Potassium Channel Blockers; 0/Potassium Channels; 0/Potassium Channels, Voltage-Gated; 0/Quaternary Ammonium Compounds; 0/Sulfanilamides; 0/Sulfonamides; 0/Trans-Activators; 115256-11-6/dofetilide; 138490-53-6/WAY 123398; 63231-63-0/RNA; 68379-02-2/clofilium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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