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

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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 studied 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‐PGF1α 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.