Competitive inhibition of mouse brain nitric oxide synthase by amiloride: A case for enzyme cross-inhibition

Paolo Ascenzi, Rodolfo Federico, Enea Menegatti, Giorgio Venturini

Research output: Contribution to journalArticle

Abstract

Amiloride, a diuretic and antihypertensive drug, inhibits Na + transporting systems, diamine oxidases and the human urinary plasminogen activator. Present results indicate that amiloride is a competitive inhibitor of mouse brain nitric oxide synthase (NOS; K(i) = 4.5 x 10 -4 M, at pH 7.5 and 37.0°C), but not a nitric oxide (NO) precursor, representing a case for enzyme cross-inhibition. The decreased levels of NO, as a consequence of NOS inhibition, might induce some clinically-adverse amiloride reactions, such as an unexpected reduced antihypertensive effect.

Original languageEnglish
Pages (from-to)507-511
Number of pages5
JournalBiochemistry and Molecular Biology International
Volume43
Issue number3
Publication statusPublished - Oct 1997

Keywords

  • Amiloride
  • Mouse brain nitric oxide synthase
  • Nitric oxide synthase inhibition

ASJC Scopus subject areas

  • Biochemistry
  • Genetics
  • Molecular Biology

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