Positive inotropic effect of endothelin-1 in the neonatal mouse right ventricle

Eur J Pharmacol. 2003 Jul 11;472(3):197-204. doi: 10.1016/s0014-2999(03)01936-8.

Abstract

In neonatal mouse right ventricles, endothelin-1 (ET-1, 1-300 nM) induced a dose-dependent increase in twitch contractions and the dose-response curve was shifted to the right by BQ-123 (10 microM), an endothelin ET(A) receptor antagonist. The ET-1 (100 nM)-induced positive inotropy was accompanied by an increase in [Ca(2+)](i) transients without any change in the [Ca(2+)](i)-force relationship. Ryanodine (1 microM) partially decreased the [Ca(2+)](i) transients and contractile force, but did not affect the ET-1 (100 nM)-induced positive inotropy. Reduction of [Na(+)](o) elicited an increase in contractile force, and this effect was significantly inhibited by KB-R7943 (30 microM), an inhibitor of the Na(+)-Ca(2+) exchanger. KB-R7943 (30 microM) almost completely suppressed the positive inotropic effect of ET-1. Activation of protein kinase C (PKC) by phorbol 12,13-dibutylate (100 nM) decreased the contractile force, an effect which was suppressed by bisindolylmaleimide I (3 microM). On the other hand, the ET-1-induced positive inotropic effect was unaffected by bisindolylmaleimide I (3 microM). These results suggest that the positive inotropic effect of ET-1 in neonatal mouse right ventricles is caused by the increase in [Ca(2+)](i) transients through activation of the endothelin ET(A) receptor and the increase in Ca(2+) influx via the Na(+)-Ca(2+) exchanger during an action potential. Furthermore, the ET-1-induced positive inotropy is independent of the effects of PKC, which makes it distinct from the ET-1-mediated pathways reported for cardiac tissues in other species.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Animals, Newborn
  • Cardiotonic Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Endothelin-1 / pharmacology*
  • Heart Ventricles / drug effects
  • In Vitro Techniques
  • Mice
  • Myocardial Contraction / drug effects*
  • Myocardial Contraction / physiology
  • Ventricular Function

Substances

  • Cardiotonic Agents
  • Endothelin-1