Berti F, Galli G, Omini C, Rossoni G, Brunelli G, Daffonchio L, Viganò T, Magni F, Crivellari M T, Forgione A
Arzneimittelforschung. 1987 Jan;37(1):27-32.
S-(+)-2-(4-Fluorophenyl)-alpha-methyl-5-benzoxazolacetic acid (flunoxaprofen, Priaxim is a new antiinflammatory compound, which in various biological systems interferes with the generation and release of arachidonic acid metabolites of the cyclo-oxygenase pathways without affecting the formation of 5- and 12-lipoxygenase products. Flunoxaprofen reduces the concentration of thromboxane (TX)B2 (ED50 = 35.4 mg/kg p.o.) and prostaglandin (PG)E2-like activity (ED50 = 39.9 mg/kg p.o.) in the inflammatory exudate of rats 8 h after implantation of sponges soaked with carrageenan, whereas the concentration of leukotriene (LT)B4 remains in the range of that of the untreated animals (3.1 ng/ml). Flunoxaprofen inhibits cell infiltration in the exudate and this suggests that LTB4 does not initiate cell recruitment but may represent a mechanism for amplifying the inflammatory response. Using human platelets challenged with collagen, flunoxaprofen only at higher concentration (10(-4) mol/l) reduces TXB2 formation without altering generation of 12-hydroxy-5,8,10,14-eicosatetraenoic acid. This suggests a low capacity of flunoxaprofen of affecting platelet aggregation regulated by arachidonic acid metabolites. Flunoxaprofen prevents pulmonary changes due to secondary release of TXA2 in the guinea-pig. In fact this drug prevents changes due to immunological reaction and antagonizes bronchoconstriction due to exogenous administration of histamine and LTC4.(ABSTRACT TRUNCATED AT 250 WORDS)
S-(+)-2-(4-氟苯基)-α-甲基-5-苯并恶唑乙酸（氟诺洛芬，普瑞昔明）是一种新型抗炎化合物，在多种生物系统中，它能干扰环氧化酶途径中花生四烯酸代谢产物的生成和释放，而不影响5-和12-脂氧合酶产物的形成。氟诺洛芬可降低角叉菜胶浸泡海绵植入大鼠8小时后炎症渗出液中血栓素（TX）B2的浓度（口服半数有效量=35.4毫克/千克）和前列腺素（PG）E2样活性（口服半数有效量=39.9毫克/千克），而白三烯（LT）B4的浓度仍处于未治疗动物的范围内（3.1纳克/毫升）。氟诺洛芬抑制渗出液中的细胞浸润，这表明LTB4不是引发细胞募集的因素，而是可能代表一种放大炎症反应的机制。在用人血小板与胶原蛋白进行刺激的实验中，氟诺洛芬仅在较高浓度（10⁻⁴摩尔/升）时才会减少TXB2的形成，而不改变12-羟基-5,8,10,14-二十碳四烯酸的生成。这表明氟诺洛芬影响由花生四烯酸代谢产物调节的血小板聚集的能力较低。氟诺洛芬可预防豚鼠因TXA2二次释放而导致的肺部变化。实际上，这种药物可预防免疫反应引起的变化，并拮抗因外源性给予组胺和LTC4而导致的支气管收缩。（摘要截选至250词）
