Endothelin ETA- and ETB-receptor-mediated vasoconstriction in rat pulmonary arteries and arterioles

J Cardiovasc Pharmacol. 1994 May;23(5):838-45. doi: 10.1097/00005344-199405000-00022.

Abstract

We investigated the endothelin (ET) receptors involved in the vasoconstrictor responses to ET-1 in rat pulmonary arteries and arterioles and the effect of endothelium removal, nitric oxide (NO) synthase inhibition, and hypoxia on ET-1-induced responses in the arteries. In isolated rat pulmonary artery rings (2-3 mm ID) prepared from the pulmonary artery branch before its entry into the lung, ET-1-induced vasoconstrictor responses. These responses were mediated by the ETA receptor as they were competitively antagonized by the ETA receptor antagonist FR 139317, and the ETB-receptor agonist sarafotoxin S6c (SXS6c) was a very weak vasoconstrictor in these vessels, inducing maximum contractions only 9% of those of ET-1. In contrast, in rat intrapulmonary resistance arteries (100-150 microns ID), SXS6c induced FR 139317-resistant contractions, and these vessels were more sensitive to SXS6c than to ET-1. SXS6c produced maximum contractions 92% those of ET-1, suggesting that ET-1-induced contractions were mediated by the ETB receptor in these resistance vessels. In the larger pulmonary arteries, the NO synthase inhibitor L-N omega nitroarginine methyl ester (L-NAME) (100 microM) potentiated responses to ET-1, an effect that was reversed by FR 139317. Endothelium removal also potentiated response to ET-1, and L-NAME had no effect on ET-1 responses in endothelium-denuded vessels, suggesting that in these vessels the ETA receptor-mediated responses to ET-1 are normally suppressed by endothelium-derived NO.(ABSTRACT TRUNCATED AT 250 WORDS)

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arginine / analogs & derivatives
  • Arginine / pharmacology
  • Arterioles / drug effects*
  • Arterioles / metabolism
  • Azepines / pharmacology
  • Dose-Response Relationship, Drug
  • Endothelin Receptor Antagonists*
  • Endothelins / pharmacology
  • Endothelium, Vascular / physiology
  • Hypoxia / pathology
  • In Vitro Techniques
  • Indoles / pharmacology
  • NG-Nitroarginine Methyl Ester
  • Nitric Oxide / antagonists & inhibitors
  • Pulmonary Artery / drug effects*
  • Pulmonary Artery / metabolism
  • Rats
  • Vasoconstriction / drug effects*
  • Vasoconstrictor Agents / pharmacology
  • Viper Venoms / pharmacology

Substances

  • Azepines
  • Endothelin Receptor Antagonists
  • Endothelins
  • Indoles
  • Vasoconstrictor Agents
  • Viper Venoms
  • sarafotoxins s6
  • FR 139317
  • Nitric Oxide
  • Arginine
  • NG-Nitroarginine Methyl Ester