Background
Misoprostol (free acid)-d5 contains five deuterium atoms at the 16 methyl, 17, and 17' positions. It is intended for use as an internal standard for the quantification of misoprostol (free acid) by GC- or LC-mass spectrometry (MS). 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 ?g/kg),2 inhibit superoxide generation in human neutrophils (EC50 = 0.35 ?M),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 ulcerationN. Engl. J. Med.3271575-1580(1992)
2.Bunce, K.T., Clayton, N.M., Coleman, R.A., et al.GR63799X - a novel prostanoid with selectivity for EP3 receptorsAdv. Prostaglandin Thromboxane Leukot. Res.21(A)379-382(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 neutrophilsBr. J. Pharmacol.114(7)1459-1465(1995)
4.Smith, G.C.S., Coleman, R.A., and McGrath, J.C.Characterization of dilator prostanoid receptors in the fetal rabbit ductus arteriosusJ. Pharmacol. Exp. Ther.271390-396(1994)
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