Aishita H, Morimura T, Obata T, Miura Y, Miyamoto T, Tsuboshima M, Mizushima Y
Arch Int Pharmacodyn Ther. 1983 Feb;261(2):316-27.
Anti-inflammatory activities of ONO-3144 have been studied in various experimental models. This compound showed an inhibitory effect on increased vascular permeability and acute inflammation. In the carrageenin test the activity of ONO-3144 was comparable to that of indomethacin (IM), while in the dextran, albumin, yeast and scald edema test it was more potent than that of IM. Unlike IM, phenylbutazone (PB) and tiaramide (TI), ONO-3144 showed marked inhibitory effects on H2O2-induced hemolysis and lipid peroxidation. In the prostaglandin (PG) biosynthesis series, ONO-3144 did not inhibit cyclooxygenase activity but stimulated PG hydroperoxidase activity, facilitated conversion to PGH2 and also inhibited thromboxane (Tx) synthetase. The findings suggest that ONO-3144 is potentially a new type of anti-inflammatory drug. Possible sites of action of ONO-3144 are discussed.
已在多种实验模型中研究了ONO - 3144的抗炎活性。该化合物对血管通透性增加和急性炎症表现出抑制作用。在角叉菜胶试验中，ONO - 3144的活性与吲哚美辛（IM）相当，而在右旋糖酐、白蛋白、酵母和烫伤水肿试验中，它比IM更有效。与IM、保泰松（PB）和替拉米特（TI）不同，ONO - 3144对H2O2诱导的溶血和脂质过氧化表现出显著的抑制作用。在前列腺素（PG）生物合成系列中，ONO - 3144不抑制环氧化酶活性，但刺激PG氢过氧化物酶活性，促进向PGH2的转化，并且还抑制血栓素（Tx）合成酶。这些发现表明ONO - 3144可能是一种新型抗炎药物。讨论了ONO - 3144可能的作用位点。
