[Inhibitory effect of 2-(2-fluoro-4-biphenylyl)propionic acid (Flurbiprofen) on prostaglandin synthesis].
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.
D000818:Animals; D001095:Arachidonic Acids / Q000494:pharmacology; D002351:Carrageenan; D002855:Chromatography, Thin Layer; D004357:Drug Synergism; D004487:Edema / Q000139:chemically induced; D005480:Flurbiprofen / Q000494:pharmacology*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D011422:Propionates / Q000494:pharmacology*; D011448:Prostaglandin Antagonists; D011453:Prostaglandins / Q000096:biosynthesis* / Q000302:isolation & purification; D011458:Prostaglandins E / Q000032:analysis / Q000494:pharmacology; D011460:Prostaglandins F / Q000032:analysis; D051381:Rats; D013270:Stomach / Q000187:drug effects
D001095:Arachidonic Acids; D011422:Propionates; D011448:Prostaglandin Antagonists; D011453:Prostaglandins; D011458:Prostaglandins E; D011460:Prostaglandins F; D005480:Flurbiprofen; D002351:Carrageenan