Fluprostenol is a metabolically stable analog of PGF2α with potent FP receptor agonist activity.1,2 Fluprostenol is the optically active enantiomer of fluprostenol and would be expected to have twice the potency as the racemic mixture. Fluprostenol inhibits PGF2α binding to human and rat FP receptors with IC50 values of 3.5 and 7.5 nM, respectively.1,2 It is a much more potent luteolytic agent than PGF2α in rats with a minimum fully effective dose of 270 µg/kg to terminate pregnancy.3 It is also an effective inhibitor of rat adipose precursor differentiation in primary cultures with an IC50 of 3-10 x 10−11 M.4
1
Abramovitz, M., Boie, Y., Nguyen, T., et al. Cloning and expression of a cDNA for the human prostanoid FP receptor. J Biol Chem2692632-2636(1994).
2
Lake, S., Gullberg, H., Wahlqvist, J., et al. Cloning of the rat and human prostaglandin F2α receptors and the expression of the rat prostaglandin F2α receptor. FEBS Lett355317-325(1994).
3
Dukes, M., Russell, W., and Walpole, A.L. Potent luteolytic agents related to prostaglandin F2α. Nature250330-331(1974).
4
Serrero, G., and Lepak, N.M. Prostaglandin F2α receptor (FP receptor) agonists are potent adipose differentiation inhibitors for primary culture of adipocyte precursors in defined medium. Biochem Biophys Res Commun233200-202(1997).