SB 234551, a novel endothelin--A receptor antagonist, unmasks endothelin-induced renal vasodilatation in the dog

J Cardiovasc Pharmacol. 1998:31 Suppl 1:S339-41. doi: 10.1097/00005344-199800001-00094.

Abstract

Infusion of endothelin-1 (ET-1) into conscious, chronically instrumented dogs (10 ng/kg.min i.v.) resulted in a significant increase in mean arterial pressure and significant reductions in renal plasma flow, glomerular filtration rate, and sodium excretion. Intravenous infusion of SB 209670 (30 micrograms/kg.min, i.v.) abolished these responses, whereas infusion of SB 234551 (30 micrograms/kg.min, i.v.) resulted in significant increases in renal plasma flow and urinary sodium excretion. These data indicate that SB 234551 can unmask ETB receptor-induced renal vasodilatation and inhibition of sodium reabsorption.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Dogs
  • Endothelin Receptor Antagonists*
  • Endothelins / pharmacology*
  • Female
  • Indans / pharmacology
  • Infusions, Intravenous
  • Kidney Function Tests
  • Natriuresis / drug effects
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Renal Circulation / drug effects*
  • Vasodilation / drug effects*

Substances

  • Endothelin Receptor Antagonists
  • Endothelins
  • Indans
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • 1H-Indene-2-carboxylic acid, 1-(1,3-benzodioxol-5-yl)-3-(2- (carboxymethoxy)-4-methoxyphenyl)-2,3-dihydro-5-propoxy-, (1S,2R,3S)-