The (+)-enantiomer is responsible for the antiplatelet and anti-inflammatory activity of (±)-indobufen

C. Cerletti, S. Manarini, M. Colombo, A. Tavani

Research output: Contribution to journalArticle

Abstract

The racemic compound indobufen and its (+) and (-)-enantiomers have been compared for their effects on blood platelet function and rat carrageenan pleurisy. The antiplatelet properties were sudied in-vitro in human platelets by measuring the inhibition of platelet aggregation and generation of serum thromboxane (Tx) B2. In-vivo, the antiplatelet and anti-inflammatory properties were studied in rats by measuring the inhibition of serum TxB2, the amount of 6-keto PGF(1α) in pleural exudate and pleural exudate volume. In all tests the (+)-enantiomer was slightly more potent than the racemate, while the (-)-enantiomer was far less potent. In the same rats, treatment with the lowest doses of the compounds giving 90% inhibition of serum thromboxane B2 generation was associated with occasional macroscopic lesions of the gastric mucosa.

Original languageEnglish
Pages (from-to)885-887
Number of pages3
JournalJournal of Pharmacy and Pharmacology
Volume42
Issue number12
Publication statusPublished - 1990

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology

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