非ステロイド性抗炎症剤EB-382の血小板凝集抑制作用

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The inhibitory effects of EB-382,a non-steroidal antiinflammatory agent, on platelet aggregation and prostaglandin biosynthesis were studied. EB-382 exhibited a dose-dependent inhibitory effect on the collagen and arachidonic acid-induced rabbit platelet aggregation in vitro, and its IC_<50> values were 231.2 and 116.1μM, respectively. The efficacy of EB-382 was about twice less potent than that of ibuprofen. EB-382 exhibited a dose-dependent inhibitory effect on the collagen-induced rat platelet aggregation ex vivo, and its ED_<50> value was 62.5mg/kg, p.o. The efficacy of EB-382 was about twice less potent than that of ibuprofen. EB-382 did not affect the ADP-induced platelet aggregation both in rabbits in vitro and rats ex vivo. EB-382 inhibited dose-dependently the arachidonic acid-induced pulmonary thrombotic mortality in mice, and its ED_<50> value was 62.9mg/kg, p.o. The efficacy of EB-382 was about twice less potent than that of ibuprofen. EB-382 exhibited a dose-dependent inhibition of prostaglandin synthetase activity, and its IC_<50> value was 1.9×10^<-4>M. The efficacy of EB-382 was about 10 times less potent than that of ibuprofen. These results indicate that EB-382 affect platelet aggregation through the inhibition of the prostaglandin biosynthesis, but its efficacy on the platelet aggregation is fairly less potent, comparing with its inflammatory, analgesic and antipyretic activities.
公益社団法人日本薬学会の論文
1987-01-25

非ステロイド性抗炎症剤EB-382の血小板凝集抑制作用

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