1. Academic Validation
  2. Phosphoramidon, a metalloproteinase inhibitor, suppresses the hypertensive effect of big endothelin-1

Phosphoramidon, a metalloproteinase inhibitor, suppresses the hypertensive effect of big endothelin-1

  • Eur J Pharmacol. 1990 Aug 21;185(1):103-6. doi: 10.1016/0014-2999(90)90216-s.
Y Matsumura 1 K Hisaki M Takaoka S Morimoto
Affiliations

Affiliation

  • 1 Department of Pharmacology, Osaka University of Pharmaceutical Sciences, Japan.
Abstract

Intravenous (i.v.) injection of big endothelin-1 (1-39, 0.05-1.0 nmol/kg) to anaesthetized rats produced a dose-dependent and long-lasting hypertensive effect, the magnitude of which was similar to that evoked by ET-1 (1-21). In Animals given phosphoramidon (0.25 mg/kg per min i.v.), a metalloproteinase inhibitor, the hypertensive effect of big endothelin-1 was markedly attenuated. The same dose of phosphoramidon did not influence the endothelin-1-induced hypertensive effect. The possibility that big endothelin-1 is converted to endothelin-1 by a phosphoramidon-sensitive metalloproteinase in vivo warrants further attention.

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