Carminati P, Lerner L J
Proc Soc Exp Biol Med. 1975 Feb;148(2):455-8. doi: 10.3181/00379727-148-38560.
Diftalone and its metabolites 7, 14-Dihydroxyphthalzino (2,3-b)phthalazine-5, 12 (7H, 14H)-dione, 7-Hydroxyphthalazino (2, 3-b)phthalzine-5,12 (7H, 14H)=DIONE, AND 12 (1(2H)-oxo-2-phthalazinyl)methylbenzoic acid inhibited prostaglandin synthesis in bovine seminal vesicle microsome preparations. Diftalone was the most active of these compounds but less active than indomethacin although more active than phenylbutazone or asprin. The magnitude of the concentration of arachidonic acid influenced the velocity of the reaction in the synthesis of prostaglandins; the highest concentrations inhibited the rate of reaction. The results of the in vitro inhibition of prostaglandin synthetase studies correlated well with those obtained in the in vivo carrageenan edema inhibition studies in the rat. The relative potencies for Diftalone, indomethacin and phenylbutazone were similar with both experimental procedures.
双氟尼酸及其代谢产物7,14 - 二羟基酞嗪并(2,3 - b)酞嗪 - 5,12(7H,14H) - 二酮、7 - 羟基酞嗪并(2,3 - b)酞嗪 - 5,12(7H,14H) - 二酮以及12 - [(1(2H) - 氧代 - 2 - 酞嗪基)甲基]苯甲酸抑制了牛精囊微粒体制剂中前列腺素的合成。双氟尼酸是这些化合物中活性最强的，但比吲哚美辛活性低，不过比保泰松或阿司匹林活性高。花生四烯酸浓度的大小影响前列腺素合成反应的速度；最高浓度抑制反应速率。前列腺素合成酶体外抑制研究的结果与大鼠体内角叉菜胶性水肿抑制研究的结果相关性良好。双氟尼酸、吲哚美辛和保泰松在两种实验方法中的相对效力相似。
