Electrophysiological and haemodynamic effects of endothelin ETA and ETB receptors in normal and ischaemic working rabbit hearts

Br J Pharmacol. 2005 Sep;146(1):118-28. doi: 10.1038/sj.bjp.0706304.

Abstract

The aims of this study were to determine if endothelin-1 (ET-1) under normal and ischaemic conditions exhibits a direct arrhythmogenic effect that is independent of its ability to cause coronary vasoconstriction, and to determine the contribution of the ET(A) and ET(B) receptor subtype. ET(A/B) (with ET-1) and ET(A) (ET-1 in the presence of BQ-788) receptor activation resulted in a significant reduction in both epi- and endocardial monophasic action potential duration (MAPD(90)). ET(A) receptor activation reduced both epi- and endocardial effective refractory period (ERP). This MAPD(90) and ERP shortening were associated with a reduction in coronary flow, myocardial contractility and induction of ventricular fibrillation (VF) during ERP measurement. The ET(B) agonist sarafotoxin (S6c) had no marked, or concentration-dependent, effect on MAPD(90), ERP, myocardial contractility or induction of arrhythmias. Neither ET-1 nor S6c, given prior to coronary artery occlusion, significantly changed the ischaemia-induced dispersion of MAPD(90), ERP or the % incidence of VF. In conclusion, neither ET(A) nor ET(B) receptor stimulation has a direct arrhythmogenic effect in isolated rabbit hearts under normal or ischaemic conditions. The ET-1-induced arrhythmogenic effect observed in nonischaemic hearts is likely to be the result of the associated coronary vasoconstriction caused by ET(A) receptor stimulation resulting in myocardial ischaemia.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Arrhythmias, Cardiac / chemically induced
  • Blood Pressure / drug effects
  • Coronary Circulation / drug effects
  • Disease Models, Animal
  • Endocardium / drug effects*
  • Endocardium / physiology
  • Endothelin B Receptor Antagonists
  • Endothelin-1 / pharmacology*
  • In Vitro Techniques
  • Male
  • Myocardial Contraction / drug effects
  • Myocardial Ischemia / physiopathology*
  • Oligopeptides / pharmacology
  • Pericardium / drug effects*
  • Pericardium / physiology
  • Piperidines / pharmacology
  • Rabbits
  • Receptor, Endothelin A / agonists*
  • Receptor, Endothelin A / physiology
  • Receptor, Endothelin B / agonists*
  • Receptor, Endothelin B / physiology
  • Ventricular Fibrillation
  • Viper Venoms / pharmacology

Substances

  • Endothelin B Receptor Antagonists
  • Endothelin-1
  • Oligopeptides
  • Piperidines
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Viper Venoms
  • sarafotoxins s6
  • BQ 788