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

作者信息

Cerletti C, Manarini S, Colombo M, Tavani A

机构信息

Istituto di Ricerche Farmacologiche Mario Negri, Santa Maria Imbaro, Italy.

出版信息

J Pharm Pharmacol. 1990 Dec;42(12):885-7. doi: 10.1111/j.2042-7158.1990.tb07049.x.

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.

摘要

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