Incomplete inhibition of endothelin-1 pressor effects by an endothelin ETA receptor antagonist

Eur J Pharmacol. 1993 Aug 24;240(2-3):295-8. doi: 10.1016/0014-2999(93)90912-2.

Abstract

Incomplete inhibition of endothelin-1-induced pressor effects by FR-139317, a novel, potent, ETA receptor antagonist, was observed in conscious, normotensive rats. Maximum inhibition by FR-139317 of the endothelin-1 pressor response (0.1, 0.3, 1.0 nmol/kg) was 49 +/- 7, 41 +/- 3, 62 +/- 5%, respectively. Two ETB-selective receptor ligands induced pressor responses in conscious rats. A portion of the endothelin-1 pressor response may be mediated by ETB receptors, and ETB-mediated vasoconstriction may contribute to incomplete inhibition of the pressor response to endothelin-1 by an ETA-selective receptor antagonist.

MeSH terms

  • Animals
  • Azepines / pharmacology*
  • Blood Pressure / drug effects*
  • Endothelin Receptor Antagonists*
  • Endothelins / antagonists & inhibitors*
  • Indoles / pharmacology*
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Vasoconstrictor Agents / pharmacology
  • Viper Venoms / pharmacology

Substances

  • Azepines
  • Endothelin Receptor Antagonists
  • Endothelins
  • Indoles
  • Vasoconstrictor Agents
  • Viper Venoms
  • sarafotoxins s6
  • FR 139317