Evidence for heterogeneity of endothelin receptor distribution in human coronary artery

Br J Pharmacol. 1993 Nov;110(3):1201-5. doi: 10.1111/j.1476-5381.1993.tb13942.x.

Abstract

1. The receptors mediating endothelin-evoked contraction of human coronary artery have been investigated in isolated segments of the left anterior descending coronary artery (LAD). 2. Endothelin-1 (ET-1) was 10 times more potent in distal than in proximal segments but the potency ratio between ET-1 and ET-3 (endothelin-3) was similar and close to 100 in any segment of the artery. 3. BQ-123, an ETA receptor antagonist, competitively antagonized the response to ET-1 of distal segments (pA2 equal to 7.47). In the proximal segments, part of the contractile response was BQ123 sensitive, but the antagonism was non-competitive. In both groups of segments, the response to ET-3 could be completely blocked by BQ-123. 4. These observations indicate that ETA receptors mediate the contractile response to ET-1 in distal, pre-resistant coronary arteries, but that other ET receptors are also involved in the contractile response of proximal segments.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Coronary Vessels / drug effects
  • Coronary Vessels / physiology
  • Coronary Vessels / ultrastructure*
  • Endothelin Receptor Antagonists
  • Endothelins / pharmacology
  • Female
  • Humans
  • In Vitro Techniques
  • Male
  • Middle Aged
  • Muscle Contraction / drug effects
  • Muscle Contraction / physiology
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / physiology
  • Muscle, Smooth, Vascular / ultrastructure
  • Peptides, Cyclic / pharmacology
  • Receptors, Endothelin / classification
  • Receptors, Endothelin / physiology*

Substances

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