Pharmacology of endothelin-1 in isolated vessels: effect of nicardipine, methylene blue, hemoglobin, and gossypol

J Cardiovasc Pharmacol. 1989:13 Suppl 5:S19-22; discussion S45.

Abstract

Sensitive bioassay tissues for porcine endothelin-1 (ET-1) were developed in a cascade superfusion system and in organ baths. Venous preparations of the rabbit and rat were more sensitive than arterial preparations. ET-1 had a different pharmacological profile than Bay K 8644 on the various preparations. Nicardipine (0.1-1 microM) abolished the responses to Bay K 8644 without affecting those induced by ET-1. Thus, ET-1 contracts venous and some arterial vessels via specific receptors or channels that differ from dihydropyridine-sensitive calcium channels. Methylene blue and hemoglobin potentiated responses to ET-1 in endothelium-denuded venous vessels, whereas gossypol had no effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester / pharmacology
  • Animals
  • Arteries / drug effects
  • Calcium Channels / drug effects
  • Calcium Channels / physiology*
  • Endothelins
  • Gossypol / pharmacology
  • Hemoglobins / pharmacology
  • In Vitro Techniques
  • Indomethacin / pharmacology
  • Male
  • Methylene Blue / pharmacology
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects*
  • Nicardipine / pharmacology
  • Peptides / antagonists & inhibitors*
  • Peptides / pharmacology
  • Rabbits
  • Rats
  • Rats, Inbred Strains
  • Veins / drug effects

Substances

  • Calcium Channels
  • Endothelins
  • Hemoglobins
  • Peptides
  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Nicardipine
  • Gossypol
  • Methylene Blue
  • Indomethacin