High potency inhibition of hERG potassium channels by the sodium–calcium exchange inhibitor KB‐R7943

BACKGROUND AND PURPOSE KB‐R7943 is an isothiourea derivative that is used widely as a pharmacological inhibitor of sodium–calcium exchange (NCX) in experiments on cardiac and other tissue types. This study investigated KB‐R7943 inhibition of hERG (human ether‐à‐go‐go‐related gene) K+ channels that u...

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Veröffentlicht in:	British journal of pharmacology 2012-04, Vol.165 (7), p.2260-2273
Hauptverfasser:	Cheng, Hongwei, Zhang, Yihong, Du, Chunyun, Dempsey, Christopher E, Hancox, Jules C
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Substitution Animals Benzyl Compounds - pharmacology Biological and medical sciences ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels - antagonists & inhibitors Ether-A-Go-Go Potassium Channels - chemistry Ether-A-Go-Go Potassium Channels - genetics HEK293 Cells hERG Humans IhERG IKr In Vitro Techniques KB‐R7943 Medical sciences Models, Molecular Mutagenesis, Site-Directed Mutant Proteins - antagonists & inhibitors Mutant Proteins - chemistry Mutant Proteins - genetics Myocytes, Cardiac - drug effects Myocytes, Cardiac - metabolism NCX Patch-Clamp Techniques Pharmacology. Drug treatments Rabbits rapid delayed rectifier K+ current Recombinant Proteins - antagonists & inhibitors Recombinant Proteins - chemistry Recombinant Proteins - genetics Research Papers Sodium-Calcium Exchanger - antagonists & inhibitors sodium–calcium exchange Thiazolidines - pharmacology Thiourea - analogs & derivatives Thiourea - pharmacology
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