Potentiation by endothelin-1 of vasoconstrictor response in stroke-prone spontaneously hypertensive rats

Eur J Pharmacol. 2001 Mar 9;415(1):45-9. doi: 10.1016/s0014-2999(01)00817-2.

Abstract

Norepinephrine-induced vasoconstriction was significantly greater in perfused mesenteric arteries of stroke-prone spontaneously hypertensive rats (SHRSPs) compared with cases of age-matched Wistar Kyoto rats (WKYs). Neither endothelin ET(A) receptor antagonist FR139317 ((R)2-[(R)-2-[(S)-2-[[1-(hexahydro-1H-azepinyl)]carbonyl]amino-4-methyl-pentanoyl] amino-3-[3-(1-methyl-1H-indoyl)]propionyl]amino-3-(2-pyridyl) propionic acid) nor endothelin ET(B) receptor antagonist BQ788 [N-cis-2,6-dimethylpiperidinocarbonyl-L-g-methylleucyl-D-1-methoxycarbonyl-tryptophanyl-D-norleucine] affected the increased responses observed in SHRSPs, suggesting that endogenous endothelin-1 is not involved in this phenomenon. Norepinephrine-induced vasoconstriction was significantly enhanced by subpressor dose of endothelin-1 (0.3 nM), both in SHRSPs and WKYs. In SHRSPs, endothelin-1-induced enhancement was abolished by FR139317, in contrast to the case with WKYs, in which BQ788 markedly suppressed endothelin-1-induced augmentation of norepinephrine responses. Our results indicate that exogenous endothelin-1 enhances contractile responses to norepinephrine in mesenteric arteries of WKYs and SHRSPs, through activation of different receptor subtypes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Azepines / pharmacology
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Endothelin Receptor Antagonists
  • Endothelin-1 / pharmacology*
  • Hypertension / physiopathology*
  • Indoles / pharmacology
  • Mesenteric Arteries / drug effects
  • Mesenteric Arteries / physiology
  • Norepinephrine / pharmacology
  • Oligopeptides / pharmacology
  • Piperidines / pharmacology
  • Rats
  • Rats, Inbred SHR
  • Rats, Inbred WKY
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Species Specificity
  • Vasoconstriction / drug effects*
  • Vasoconstrictor Agents / pharmacology

Substances

  • Azepines
  • Endothelin Receptor Antagonists
  • Endothelin-1
  • Indoles
  • Oligopeptides
  • Piperidines
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Vasoconstrictor Agents
  • FR 139317
  • BQ 788
  • Norepinephrine