Effect of E4031, a class III antiarrhythmic drug, on ischemia- and reperfusion-induced arrhythmias in isolated rat hearts

Jpn Heart J. 1998 Mar;39(2):183-97. doi: 10.1536/ihj.39.183.

Abstract

The delayed outward rectifier K+ channel has a role in the increase in automaticity of myocytes under pathophysiological conditions. The purpose of the present study was to clarify the effect of blockade of outward rectifier K+ channels by a class III antiarrhythmic drug, E4031, on ischemia- and reperfusion-induced arrhythmias. Ion fluxes, energy metabolites and cardiac function were measured and the epicardial electrocardiograms of Langendorff-perfused rat hearts were recorded during initial perfusion, global or regional ischemia and reperfusion. 10(-7) M of E4031 administered during the initial perfusion did not prolong the QT interval, but slowed the heart rate (

Control: 222, E4031: 183 bpm, p < 0.05), increased myocardial 45Ca2+ uptake (

Control: 2.1, E4031: 2.9 mumol/g dwt, p < 0.05) and attenuated the loss of intracellular K+ during ischemia (

Control: 238, E4031: 248 mumol/g dwt, p < 0.05). E4031 tended to reduce ischemia-induced ventricular tachyarrhythmias (

Control: 60, E4031: 30%, n.s.), but reperfusion-induced ventricular tachyarrhythmias were sustained longer by the administration of E4031 (CONTROL: 255, E4031: 623 sec, p < 0.05). Prior exposure to E4031 decreased the depletion of high energy phosphates during ischemia, but suppressed their recovery during reperfusion. These results suggest that the attenuated loss of K+ from the ischemic myocardium and the decrease in heart rate by E4031 contributed to the reduction of ischemia-induced arrhythmias. However, the increase in myocardial Ca2+ uptake and altered energy metabolism may be responsible for the increase in reperfusion-induced arrhythmias.

MeSH terms

  • Animals
  • Anti-Arrhythmia Agents / pharmacology
  • Anti-Arrhythmia Agents / therapeutic use*
  • Arrhythmias, Cardiac / drug therapy*
  • Arrhythmias, Cardiac / physiopathology
  • Calcium / metabolism
  • Energy Metabolism / drug effects
  • Heart / drug effects*
  • In Vitro Techniques
  • Male
  • Myocardial Reperfusion Injury / drug therapy*
  • Myocardial Reperfusion Injury / physiopathology
  • Myocardium / metabolism
  • Piperidines / pharmacology
  • Piperidines / therapeutic use*
  • Potassium Channels / drug effects
  • Pyridines / pharmacology
  • Pyridines / therapeutic use*
  • Rats
  • Rats, Sprague-Dawley
  • Ventricular Function, Left / drug effects

Substances

  • Anti-Arrhythmia Agents
  • Piperidines
  • Potassium Channels
  • Pyridines
  • E 4031
  • Calcium