THE (+)-ENANTIOMER IS RESPONSIBLE FOR THE ANTIPLATELET AND ANTIINFLAMMATORY ACTIVITY OF (+/-)-INDOBUFEN

被引：23

作者：

CERLETTI, C ^{[1
]}

MANARINI, S ^{[1
]}

COLOMBO, M ^{[1
]}

TAVANI, A ^{[1
]}

机构：

[1] OPIOID NEUROPHARMACOL UNIT,I-20157 MILAN,ITALY

来源：

JOURNAL OF PHARMACY AND PHARMACOLOGY | 1990年 / 42卷 / 12期

关键词：

D O I：

10.1111/j.2042-7158.1990.tb07049.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

页码：885 / 887

页数：3

共 10 条

[1] INDOBUFEN, A NEW INHIBITOR OF PLATELET-AGGREGATION - STUDIES IN GUINEA-PIGS [J].