Misoprostol (free acid)

米索前列醇是一种前列腺素E1（Cayman_13010）类似物，具有由EP2、EP3和EP4受体介导的激动剂活性。研究表明，它能够抑制大鼠胃病变的形成（ED50=0.31µg/kg）、抑制人中性粒细胞中的超氧化物生成（EC50=0.35µM）并以浓度依赖性方式舒张胎儿兔动脉导管（EC50=0.36nM）。米索前列醇在临床医学中常用于预防消化性溃疡病。它还与米非司酮（RU-486；Cayman_10006317）联合用于口服诱导妊娠早期流产。米索前列醇含有C-1甲酯，在人体内易于吸收并快速水解为活性游离酸。Misoprostol is a prostaglandin E1 (Cayman_13010) analog with agonist activity mediated by EP2, EP3, and EP4 receptors. It has been shown to inhibit the formation of gastric lesions in rats (ED50 = 0.31 µg/kg), inhibit superoxide generation in human neutrophils (EC50 = 0.35 µM), and relax fetal rabbit ductus arteriosus (EC50 = 0.36 nM) in a concentration dependent manner. Misoprostol is commonly used in clinical medicine for the prevention of peptic ulcer disease. It has also been used in conjunction with mifepristone (RU-486; Cayman_10006317) for the oral induction of first trimester abortion. Misoprostol contains a C-1 methyl ester and is readily absorbed and rapidly hydrolyzed in humans to the active free acid.