Masumoto S, Masuda C
Nihon Yakurigaku Zasshi. 1976 Nov;72(8):1025-31. doi: 10.1254/fpj.72.1025.
Inhibitory effects of 2-(2-fluoro-4-biphenylyl) propionic acid (Flurbiprofen, FP-70) on prostaglandin (PG) synthesis and PG activity were investigated both in vivo and in vitro. FP-70 at 0.64 micronM showed 50% inhibitory effect on PG synthesis from arachidonic acid in cell-free homogenate of guinea pig lung. PGE2 and PGF2alpha in the sample of lung homogenate incubated with arachidonic acid were separated by thin-layer chromatography in solvent AI system. FP-70 inhibited strongly both synthesis of PGE2 and PGF2alpha at 3 micron, but inhibited more extensively the synthesis of PGE2 than that of PGF2alpha at 0.3 micronM. FP-70 at 1 mg/kg, p.o. inhibited mostly arachidonic acid potentiation of carrageenin-induced edema in the rat paw, but did not inhibit PGE2 potentiation of carrageenin-induced edema. FP-70 also did not inhibit the contraction of rat stomach strip induced by PGE2. From the above and previously5) reported results, FP-70 proved to inhibit PG synthesis but not PG activity. It is suggested that the potent anti-inflammatory action of FP-70 is the result of inhibition of PG synthesis.
研究了2-(2-氟-4-联苯基)丙酸（氟比洛芬，FP-70）在体内和体外对前列腺素（PG）合成及PG活性的抑制作用。在豚鼠肺无细胞匀浆中，0.64微摩尔的FP-70对花生四烯酸合成PG显示出50%的抑制作用。用溶剂AI系统通过薄层色谱法分离与花生四烯酸一起孵育的肺匀浆样品中的PGE2和PGF2α。3微摩尔的FP-70强烈抑制PGE2和PGF2α的合成，但在0.3微摩尔时，对PGE2合成的抑制作用比对PGF2α合成的抑制作用更广泛。口服1毫克/千克的FP-70主要抑制角叉菜胶诱导的大鼠爪水肿中花生四烯酸的增强作用，但不抑制角叉菜胶诱导的水肿中PGE2的增强作用。FP-70也不抑制PGE2诱导的大鼠胃条收缩。根据上述及之前5）报道的结果，FP-70被证明可抑制PG合成，但不抑制PG活性。提示FP-70强大的抗炎作用是抑制PG合成的结果。
