Yamamoto S, Higuchi Y
Nihon Yakurigaku Zasshi. 1980 Jan;76(1):45-9.
Effect of 2-(2-fluoro-4-biphenylyl) propionic acid(Flurbiprofen, FP-70) on increased vascular permeability was studied using the potentiation of bradykinin-induced vascular permeability by prostaglandin in the guinea pig skin, as the test system. Prostaglandin E1 or E2 (1 microgram/site) alone did not show increased vascular permeability but did enhance the effect of various concentrations of bradykinin when concomitantly applied, whereas prostaglandin F2 alpha did not potentiate the effect of bradykinin on vascular permeability. Arachidonic acid (100 microgram/site) had no effect on vascular permeability when injected alone or in combination with bradykinin. However, arachidonic acid enhanced the effect of bradykinin when given 30 min before bradykinin. FP-70 had no inhibitory effect on prostaglandin E1 potentiation of bradykinin-induced vascular permeability. On the other hand, FP-70 completely abolished the enhancement of the effect of bradykinin by arachidonic acid. These results strongly suggest that anti-vascular permeability action of FP-70 may be due to inhibition of prostaglandin synthetase. Indomethacin and acetylsalicylic acid also exhibit similar effects. However, the inhibitory effect of FP-70 was 12.5 and 166.7 times as potent as indomethacin and acetylsalicylic acid, respectively.
以前列腺素增强缓激肽诱导的豚鼠皮肤血管通透性作为测试系统，研究了2-（2-氟-4-联苯基）丙酸（氟比洛芬，FP - 70）对血管通透性增加的影响。单独使用前列腺素E1或E2（1微克/部位）不会使血管通透性增加，但与各种浓度的缓激肽同时应用时，会增强缓激肽的作用，而前列腺素F2α不会增强缓激肽对血管通透性的作用。花生四烯酸（100微克/部位）单独注射或与缓激肽联合注射时对血管通透性均无影响。然而，在缓激肽注射前30分钟给予花生四烯酸会增强缓激肽的作用。FP - 70对前列腺素E1增强缓激肽诱导的血管通透性没有抑制作用。另一方面，FP - 70完全消除了花生四烯酸对缓激肽作用的增强。这些结果强烈表明，FP - 70的抗血管通透性作用可能是由于抑制了前列腺素合成酶。吲哚美辛和乙酰水杨酸也表现出类似的作用。然而，FP - 70的抑制作用分别是吲哚美辛和乙酰水杨酸的12.5倍和166.7倍。
