The effects of endothelin-1 on the PKA-dependent Cl- current in the heart

Jpn J Physiol. 1994:44 Suppl 2:S227-30.

Abstract

The effects of endothelin-1 (ET-1) on whole-cell cardiac PKA-dependent Cl- currents (ICl) were investigated using patch clamp techniques. ET-1 inhibited the isoproterenol-induced ICl with a half-maximally effective concentration of approximately 1 nM. ET-1 also inhibited the forskolin-induced current in a similar concentration range. The effects of ET-1 were abolished by pre-treatment of the cells with pertussis toxin. Since ET-1 was ineffective at inhibiting the ICl induced by internal dialysis with cyclic AMP, it is unlikely that the Gi-protein had a direct effect on channel gating or phosphorylation of the channel by PKA. It is concluded that ET-1 inhibited the cardiac PKA-dependent ICl by attenuating activation of adenylate cyclase and that this effect was mediated by a pertussis toxin-sensitive G-protein, presumably Gi.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylate Cyclase Toxin
  • Animals
  • Chloride Channels / drug effects*
  • Cyclic AMP-Dependent Protein Kinases / pharmacology
  • Endothelins / pharmacology*
  • Evoked Potentials / drug effects
  • Heart / drug effects*
  • Isoproterenol / pharmacology
  • Pertussis Toxin
  • Virulence Factors, Bordetella / toxicity

Substances

  • Adenylate Cyclase Toxin
  • Chloride Channels
  • Endothelins
  • Virulence Factors, Bordetella
  • Pertussis Toxin
  • Cyclic AMP-Dependent Protein Kinases
  • Isoproterenol