Inhibition of the cardiac protein kinase A-dependent chloride conductance by endothelin-1

Nature. 1994 Jul 28;370(6487):297-300. doi: 10.1038/370297a0.

Abstract

Endothelin-1 is a peptide hormone constitutively secreted by vascular and endocardial endothelial cells. Secretion of endothelin-1 is increased under certain pathophysiological conditions, including coronary vasospasm, cardiac ischaemia and myocardial infarction. We have examined the effect of endothelin-1 on the protein kinase A (PKA)-dependent chloride current in voltage-clamped guinea pig ventricular myocytes. This conductance, induced by catecholamines through beta-adrenergic receptors, counteracts the simultaneously increased L-type calcium current by shortening the action potential duration. We report here that endothelin-1, acting through ETA (endothelin-1-selective) receptors, inhibited the current through a pertussis toxin-sensitive mechanism, analogous to muscarinic receptors, by reducing the intracellular cyclic AMP concentration. This effect of endothelin-1 should help protect the ventricle against potentially arrhythmogenic shortening of the action potential during ischaemia when the circulating levels of catecholamines are increased.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cells, Cultured
  • Chlorides / metabolism*
  • Cyclic AMP / metabolism
  • Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors*
  • Endothelins / metabolism
  • Endothelins / pharmacology*
  • Guinea Pigs
  • Isoproterenol / pharmacology
  • Membrane Potentials
  • Myocardium / enzymology*
  • Peptides, Cyclic / pharmacology
  • Pertussis Toxin
  • Receptors, Endothelin / drug effects
  • Receptors, Endothelin / metabolism
  • Virulence Factors, Bordetella / pharmacology

Substances

  • Chlorides
  • Endothelins
  • Peptides, Cyclic
  • Receptors, Endothelin
  • Virulence Factors, Bordetella
  • Cyclic AMP
  • Pertussis Toxin
  • Cyclic AMP-Dependent Protein Kinases
  • Isoproterenol
  • cyclo(Trp-Asp-Pro-Val-Leu)