Literature DB >> 1983157

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

C Cerletti1, S Manarini, M Colombo, A Tavani.   

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-PGF1 alpha 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.

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Year:  1990        PMID: 1983157     DOI: 10.1111/j.2042-7158.1990.tb07049.x

Source DB:  PubMed          Journal:  J Pharm Pharmacol        ISSN: 0022-3573            Impact factor:   3.765


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  4 in total

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