Endothelin-1 does not mediate hypoxic vasoconstriction in canine isolated blood vessels: effect of BQ-123

Br J Pharmacol. 1993 Feb;108(2):418-21. doi: 10.1111/j.1476-5381.1993.tb12819.x.

Abstract

1. The role of endothelin-1 in mediating the phenomenon of hypoxic vasoconstriction was examined in canine, isolated pulmonary, circumflex coronary and femoral arterial rings. 2. In tissues with an intact endothelium, the exogenous application of endothelin-1 (0.1-300 nM) caused concentration-dependent increases in canine, isolated pulmonary artery tone. Endothelin-3 (1-300 nM) was approximately 30 fold less potent than endothelin-1 as a vasoconstrictor in this tissue. In contrast, the selective ETB-receptor agonist, sarafotoxin S6c (0.01-1 microM), failed to elicit vasoconstriction in this tissue. Thus, endothelin isopeptide-induced vasoconstriction of the canine isolated pulmonary artery is mediated exclusively by the ETA-receptor subtype. 3. The concentration-dependent increases in isometric tension induced by endothelin-1 (0.1-300 nM) were antagonized by the ETA-selective antagonist, BQ-123 (10 microM); this concentration of antagonist caused a shift to the right in the concentration-response curve for endothelin-1 of approximately two orders of magnitude. This concentration of BQ-123 did not unmask any ETB-receptor-mediated vasoconstriction since sarafotoxin S6c (0.01-1 microM) still failed to elicit contraction in the presence of this concentration of BQ-123. 4. The hypoxia-induced vasoconstriction of canine, isolated pulmonary, circumflex coronary and femoral arterial rings was unaffected by pretreatment with the endothelin receptor antagonist, BQ-123 (10 microM), a concentration shown previously to antagonize the contractile actions of exogenously applied endothelin-1 in the isolated pulmonary artery. 5. These results are the first to provide direct evidence showing that the endothelium-dependent vasoconstriction observed during acute periods of hypoxia in vitro is not mediated by an endothelin-related isopeptide.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Blood Vessels / drug effects*
  • Blood Vessels / physiology
  • Dogs
  • Endothelins / physiology*
  • Hypoxia / physiopathology*
  • In Vitro Techniques
  • Male
  • Molecular Sequence Data
  • Peptides, Cyclic / pharmacology*
  • Vasoconstriction / drug effects*
  • Vasoconstriction / physiology

Substances

  • Endothelins
  • Peptides, Cyclic
  • cyclo(Trp-Asp-Pro-Val-Leu)