Human endothelin ETA receptor antisense oligodeoxynucleotides inhibit endothelin-1 evoked vasoconstriction

Eur J Pharmacol. 1994 Aug 22;261(3):281-4. doi: 10.1016/0014-2999(94)90118-x.

Abstract

Antisense oligodeoxynucleotides to endothelin ETA receptor mRNA were used to characterize vascular smooth muscle receptors. The concentration-response curve showed a significant attenuation of endothelin-1-induced contraction in circular segments of the human superficial temporal artery. Endothelin ETB receptor antisense or mismatch oligodeoxynucleotides showed no alteration of the endothelin-1-induced contraction. Complementary experiments with the selective endothelin ETA receptor antagonist FR139317 demonstrated a shift of the concentration-response curve to the right in a competitive manner (pA2 = 6.93). The specific method of using the receptor antisense oligodeoxynucleotides approach revealed the presence of endothelin ETA receptors mediating contraction in the human superficial temporal artery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Azepines / pharmacology
  • Base Sequence
  • Endothelin Receptor Antagonists
  • Endothelins / antagonists & inhibitors*
  • Endothelins / pharmacology
  • Humans
  • In Vitro Techniques
  • Indoles / pharmacology
  • Molecular Sequence Data
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Oligonucleotides, Antisense / pharmacology*
  • RNA, Messenger / metabolism
  • Receptors, Endothelin / metabolism*
  • Vasoconstriction / drug effects*

Substances

  • Azepines
  • Endothelin Receptor Antagonists
  • Endothelins
  • Indoles
  • Oligonucleotides, Antisense
  • RNA, Messenger
  • Receptors, Endothelin
  • FR 139317