Inhibition of the human ether‐a‐go‐go‐related gene (HERG) potassium channel by cisapride: affinity for open and inactivated states

Cisapride is a prokinetic agent which has been associated with QT prolongation, torsades de pointes and cardiac arrest. The cellular mechanism for these observations is high affinity blockade of IKr (encoded by HERG). In a chronic transfection model using CHO‐K1 cells, cisapride inhibited HERG tail...

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Veröffentlicht in:	British journal of pharmacology 1999-09, Vol.128 (2), p.444-450
Hauptverfasser:	Walker, B D, Singleton, C B, Bursill, J A, Wyse, K R, Valenzuela, S M, Qiu, M R, Breit, S N, Campbell, T J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences cardiac arrhythmia Cation Transport Proteins Chinese hamster ovary (CHO‐K1) cell CHO Cells Cisapride Cisapride - pharmacology Cricetinae DNA-Binding Proteins Drug toxicity and drugs side effects treatment ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels Gastrointestinal Agents - pharmacology human ether‐a‐go‐go‐related gene (HERG) Humans Ion Channel Gating - drug effects Kinetics Medical sciences Patch-Clamp Techniques Pharmacology. Drug treatments Potassium Channel Blockers Potassium Channels - metabolism Potassium Channels, Voltage-Gated Temperature torsades de pointes Toxicity: cardiovascular system Trans-Activators Transcriptional Regulator ERG
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