Misoprostol

Misoprostol is an analog of prostaglandin E1 (PGE1; Item No. 13010) and an agonist of the PGE2 receptor subtypes EP2 and EP3.{8322,1752,59038} It binds to EP1, EP2, EP3-III, and EP4 receptors (Kis = 35.675, 10.249, 0.319, 5.499 ?M, respectively) and is selective for EP receptors over DP, FP, IP, and TP receptors (Kis = >100 ?M for all).{8322} 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.{59038,3411} It inhibits FMLP-induced superoxide anion generation in human neutrophils (EC50 = 0.35 ?M).{1752} Misoprostol inhibits ethanol-induced gastric lesion formation in rats (ED50 = 0.31 ?g/kg).{1754} Formulations containing misoprostol have been used in the prevention of NSAID-induced gastric ulcers.