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

Mikael Adner, David Erlinge, Leif G. Salford, Frances Yee, Claes Wahlestedt, Lars Edvinsson

Research output: Contribution to journalArticle

14 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)281-284
Number of pages4
JournalEuropean Journal of Pharmacology
Volume261
Issue number3
DOIs
StatePublished - Aug 22 1994
Externally publishedYes

Keywords

  • Antisense oligodeoxynucleotide
  • Endothelin ET receptor
  • Temporal artery, human

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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