Comparison of a novel ETA receptor antagonist and phosphoramidon in renal ischemia

Pharmacology. 1995 Jan;50(1):9-23. doi: 10.1159/000139262.

Abstract

Infusion (0.46 mumol/kg/min) of the endothelin (ET)-converting-enzyme inhibitor, phosphoramidon (P), protected function and structure after 30 min renal ischemia in rats more than treatment (5 mumol/kg/min) with the ETA receptor antagonist, BMS-182874 (B). The glomerular filtration rate (GFR; 0.7 +/- 0.12 ml/min) and renal plasma flow (RPF) decreased approximately 40% at 2 h reflow versus controls (C: 1.2 +/- 0.12). B weakly protected the GFR (0.8 +/- 0.07 ml/min); P restored it (1.1 +/- 0.05). Both compounds reduced tubular injury at 2 h reflow; P ameliorated glomerular changes. At 24 h the GFR (0.6 +/- 0.06 ml/min) and RPF decreased 67% versus C (1.8 +/- 0.08). B did not protect the GFR and RPF. P partially protected the GFR (0.9 +/- 0.07 ml/min) but not RPF, and reduced tubular injury. The results suggest that both ETA and non-ETA receptors mediate ET-induced changes in ischemic renal failure.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Creatinine / blood
  • Dansyl Compounds / pharmacology*
  • Endothelin Receptor Antagonists*
  • Glomerular Filtration Rate / drug effects
  • Glycopeptides / pharmacology*
  • Iodine Radioisotopes
  • Ischemia / drug therapy*
  • Kidney / blood supply*
  • Kidney / physiopathology
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Renal Plasma Flow / drug effects
  • Time Factors

Substances

  • Dansyl Compounds
  • Endothelin Receptor Antagonists
  • Glycopeptides
  • Iodine Radioisotopes
  • 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide
  • Creatinine
  • phosphoramidon