Kovács L, Falkay G
Experientia. 1981 Nov 15;37(11):1182-3. doi: 10.1007/BF01989908.
The effects of etamsylate on prostaglandin (PG) biosynthesis in microsomes of pregnant human myometrium in vitro have been determined, and compared with those of indomethacin. Both drugs inhibited PG biosynthesis, indomethacin being the more potent inhibitor of the two. Etamsylate inhibited synthesis of 6-oxo-PGF1 alpha, PGF2 alpha, PGE2, and thromboxane B2; increasing the concentration of etamsylate increased the inhibition of synthesis. It is suggested that etamsylate has no anti-cyclo-oxygenase activity, but acts by inhibiting the activity of prostacyclin synthetase, endoperoxide reductase, endoperoxide isomerase, and thromboxane synthetase.
已测定酚磺乙胺对体外妊娠人子宫肌层微粒体中前列腺素(PG)生物合成的影响,并与吲哚美辛的影响进行了比较。两种药物均抑制PG生物合成,吲哚美辛是两者中更有效的抑制剂。酚磺乙胺抑制6-氧代-PGF1α、PGF2α、PGE2和血栓素B2的合成;增加酚磺乙胺的浓度会增强对合成的抑制作用。提示酚磺乙胺没有抗环氧化酶活性,而是通过抑制前列环素合成酶、内过氧化物还原酶、内过氧化物异构酶和血栓素合成酶的活性发挥作用。