Misoprostol is a PGE1 analog with agonist activity mediated by EP2, EP3, and EP4 receptors.1,2,3,4 It has been shown to inhibit the formation of gastric lesions in rats (ED50 = 0.31 µg/kg),2 inhibit superoxide generation in human neutrophils (EC50 = 0.35 µM),3 and relax fetal rabbit ductus arteriosus (EC50 = 0.36 nM)4 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 RU-486 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.1
1
Walt, R.P. Misoprostol for the treatment of peptic ulcer and antiinflammatory-drug-induced gastroduodenal ulceration. N Engl J Med3271575-1580(1992).
2
Bunce, K.T., Clayton, N.M., Coleman, R.A., et al. GR63799X - a novel prostanoid with selectivity for EP3 receptors. Adv Prostaglandin Thromboxane Leukot Res21379-382(1990).
3
Talpain, E., Armstrong, R.A., Coleman, R.A., et al. Characterization of the PGE receptor subtype mediating inhibition of superoxide production in human neutrophils. Br J Pharmacol1141459-1465(1995).
4
Smith, G.C.S., Coleman, R.A., and McGrath, J.C. Characterization of dilator prostanoid receptors in the fetal rabbit ductus arteriosus. J Pharmacol Exp Ther271390-396(1994).
Smith, G.C.S., Coleman, R.A., and McGrath, J.C. Characterization of dilator prostanoid receptors in the fetal rabbit ductus arteriosus. J Pharmacol Exp Ther271390-396(1994).
Walt, R.P. Misoprostol for the treatment of peptic ulcer and antiinflammatory-drug-induced gastroduodenal ulceration. N Engl J Med3271575-1580(1992).
Talpain, E., Armstrong, R.A., Coleman, R.A., et al. Characterization of the PGE receptor subtype mediating inhibition of superoxide production in human neutrophils. Br J Pharmacol1141459-1465(1995).
Bunce, K.T., Clayton, N.M., Coleman, R.A., et al. GR63799X - a novel prostanoid with selectivity for EP3 receptors. Adv Prostaglandin Thromboxane Leukot Res21379-382(1990).