Differential effects of itanoxone - A new hypolipidemic and hypouricemic drug - On platelet and vascular prostaglandin generation in rats

M. Livio, C. Palmier, S. Villa, B. Maynadier, A. Delhon, H. Lauressergues, G. De Gaetano

Research output: Contribution to journalArticlepeer-review

Abstract

Itanoxone ((chloro-2′-diphenyl)-4 oxo-4 methylene 2-butyric acid), a newly developed, hypolipidemic and hypouricemic compound with moderate anti-inflammatory activity, showed a short-lived, dose-dependent (20-200 mg/kg, orally), apparently competitive inhibition of platelet malondialdehyde (MDA), stimulated by either thrombin or arachidonic acid. Repeated doses did not result in any cumulative effect. At doses which completely blocked MDA production, itanoxone also inhibited thrombin-stimulated thromboxane B2 production in platelets but had no measurable effect on vascular prostacyclin generation. Pretreatment with itanoxone partially prevented the inhibitory effect of aspirin on both platelet and vascular prostaglandin synthesis. This suggests that itanoxone - like aspirin - acts at the level of cyclo-oxygenase but with greater selectivity on the platelet enzyme. This pharmacological activity is of great theoretical interest for the potential use of this compound as an antithrombic drug.

Original languageEnglish
Pages (from-to)469-477
Number of pages9
JournalAtherosclerosis
Volume39
Issue number4
DOIs
Publication statusPublished - 1981

Keywords

  • Aspirin
  • Drug interaction
  • Itanoxone
  • Platelets
  • Prostaglandins
  • Vascular cells

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine

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