Functional coupling of ETA receptor with Ca(2+)-permeable nonselective cation channel in mouse fibroblasts and rabbit aortic smooth-muscle cells

J Cardiovasc Pharmacol. 1995:26 Suppl 3:S258-61.

Abstract

Endothelin-1 (ET-1) induces persistent vasoconstriction via a sustained increase in intracellular free Ca2+ concentrations ([Ca2+]i). The mechanisms of the elevation of [Ca2+]i operating at physiologically low concentrations of ET-1 are controversial. Here we report that both native ETA receptors in vascular smooth-muscle cells and recombinant ET(A) receptors expressed in mouse fibroblasts (Ltk cells) are functionally coupled with a non-selective cation channel, which is permeable to Ca2+ and is blocked by mefenamic acid. The channel is persistently activated by a low concentration of ET-1 (10(-10) M) without stimulation of inositol triphosphate (IP3) formation and mediates sustained vasoconstriction.

MeSH terms

  • Animals
  • Calcium / metabolism*
  • Endothelins / pharmacology*
  • Humans
  • Inositol 1,4,5-Trisphosphate / biosynthesis
  • Ion Channels / drug effects*
  • Ion Channels / physiology
  • Mefenamic Acid / pharmacology
  • Mice
  • Muscle, Smooth, Vascular / metabolism
  • Rabbits
  • Receptor, Endothelin A
  • Receptors, Endothelin / physiology*

Substances

  • Endothelins
  • Ion Channels
  • Receptor, Endothelin A
  • Receptors, Endothelin
  • Mefenamic Acid
  • Inositol 1,4,5-Trisphosphate
  • Calcium