Misoprostol-d5 is intended for use as an internal standard for the quantification of misoprostol by GC- or LC-MS. Misoprostol is an analog of prostaglandin E1 and an agonist of the PGE2 receptor subtypes EP2 and EP3.1,2,3 It binds to EP1, EP2, EP3-III, and EP4 receptors (Kis = 35.675, 10.249, 0.319, 5.499 μM, respectively) and is selective for EP receptors over DP, FP, IP, and TP receptors (Kis = >100 μM for all).1 Misoprostol inhibits electrically induced twitch contraction in isolated guinea pig ileum circular muscle and vas deferens (EC50s = 102.92 and 4.3 nM, respectively), which endogenously express high levels of EP2 and EP3 receptors, respectively.3,4 It inhibits FMLP-induced superoxide anion generation in human neutrophils (EC50 = 0.35 μM).2 Misoprostol inhibits ethanol-induced gastric lesion formation in rats (ED50 = 0.31 μg/kg).5 Formulations containing misoprostol have been used in the prevention of NSAID-induced gastric ulcers.
1.Abramovitz, M., Adam, M., Boie, Y., et al.The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogsBiochim. Biophys. Acta1483(2)285-293(2000) 2.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) 3.Savage, M.A., Moummi, C., Karabatsos, P.J., et al.SC-46275: A potent and highly selective agonist at the EP3 receptorProstaglandins Leukot. Essent. Fatty Acids49(6)939-943(1993) 4.Nials, A.T., Coleman, R.A., Hartley, D., et al.AH13205 - a novel selective prostanoid EP2 agonistBr. J. Pharmacol.10224P(1991) 5.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)