ETA-dependent pressor effects and release of prostacyclin induced by endothelins in pulmonary and renal vasculature

J Cardiovasc Pharmacol. 1993:22 Suppl 8:S235-8. doi: 10.1097/00005344-199322008-00063.

Abstract

BQ-123, a selective endothelin A (ETA) receptor antagonist, was used to study the receptors involved in the ET-1-induced release of prostacyclin (PGI2) in perfused rat lung and rabbit kidney and the pressor effects of ET-1 in rabbit renal vasculature. In perfused rat lung, infusion of ET-1 (5 nM) significantly increased the release of PGI2, which was markedly reduced after a 15-min infusion of BQ-123 (1 microM). In rabbit kidney, the PGI2 release induced by ET-1 (10 nM) was abolished by a 15-min pretreatment with BQ-123 (1 microM). In both preparations the ET-1-induced release of PGI2 was fully restored 60 min after the interruption of BQ-123 infusion. In rabbit kidney a dose-dependent increase of perfusion pressure was also observed after bolus injections of ET-1 (5 and 10 pmol). The pressor responses to ET-1 were abolished by BQ-123 (0.1 microM), and 60 min after interruption of the infusion of the antagonist, the responses to ET-1 were restored to 68% and 99% of control values, respectively. Two selective ETB receptor agonists, IRL 1620 and BQ-3020, were inactive as pressor and prostanoid-releasing agents at doses and concentration 25-50 times higher than for ET-1 in perfused rabbit kidney. A higher concentration of BQ-123 (1 microM) did not modify the pressor responses to angiotensin II (5 nmol). Our results support the hypothesis that ET-1-induced release of vasodilatory prostanoids from perfused rat lung and rabbit kidney and constriction of rabbit renal vasculature are triggered by activation of ETA receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Endothelin Receptor Antagonists
  • Endothelins / pharmacology*
  • Epoprostenol / metabolism*
  • In Vitro Techniques
  • Male
  • Peptide Fragments / pharmacology
  • Peptides, Cyclic / pharmacology
  • Pulmonary Circulation / drug effects*
  • Rabbits
  • Rats
  • Rats, Wistar
  • Receptors, Endothelin / drug effects
  • Receptors, Endothelin / physiology*
  • Renal Circulation / drug effects*

Substances

  • Endothelin Receptor Antagonists
  • Endothelins
  • Peptide Fragments
  • Peptides, Cyclic
  • Receptors, Endothelin
  • sovateltide
  • Epoprostenol
  • cyclo(Trp-Asp-Pro-Val-Leu)