ONO-3144, a new anti-inflammatory drug and its possible mechanism of action.

ONO-3144, a new anti-inflammatory drug and its possible mechanism of action.
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ONO-3144,一种新型抗炎药及其可能的作用机制。

DOI:
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发表时间:
1983
影响因子:
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通讯作者:
Y. Mizushima
Y. Mizushima
中科院分区:
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文献类型:
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作者:
H. Aishita;T. Morimura;T. Obata;Y. Miura;T. Miyamoto;M. Tsuboshima;Y. Mizushima

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ONO-3144 的抗炎活性已在各种实验模型中进行了研究。该化合物对血管通透性增加和急性炎症具有抑制作用。在角叉菜胶测试中,ONO-3144 的活性与吲哚美辛 (IM) 相当,而在葡聚糖、白蛋白、酵母和烫伤水肿测试中,ONO-3144 的活性比 IM 更有效。与 IM、保泰松 (PB) 和噻拉胺 (TI) 不同,ONO-3144 对 H2O2 诱导的溶血和脂质过氧化表现出显着的抑制作用。在前列腺素(PG)生物合成系列中,ONO-3144不抑制环氧合酶活性,而是刺激PG氢过氧化物酶活性,促进转化为PGH2并抑制血栓素(Tx)合成酶。研究结果表明ONO-3144可能是一种新型抗炎药。讨论了 ONO-3144 可能的作用位点。
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.