Sulprostone is a metabolism resistant synthetic analog of PGE₂.¹ It is a selective agonist for EP₃ receptors with a K_i value of 0.35 nM at the human recombinant EP₃-III receptor and an IC₅₀ of 0.01 µM for the inhibition of PGE₂ binding.^2,3 Sulprostone is a potent stimulator of uterine smooth muscle contractions with high abortifacient activity.^4,5

1 Schaaf, T.K., Bindra, J.S., Eggler, J.F., et al. N-(methanesulfonyl)-16-phenoxyprostaglandincarboxamides: Tissue-selective, uterine stimulants. J Med Chem 24 1353-1359 (1981).

2 Abramovitz, M., Adam, M., Boie, Y., et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta 1483 285-293 (2000).

3 Negishi, M., Harazono, A., Sugimoto, Y., et al. TEI-3356, a highly selective agonist for the prostaglandin EP₃ receptor. Prostaglandins 48 275-283 (1994).

4 Schillinger, E., Prior, G., Speckenbach, A., et al. Receptor binding in various tissues of PGE₂, and sulprostone, a novel PGE₂-derivative. Prostaglandins 18 293-302 (1979).

5 Krishna, U., Gupta, A.N., Ma, H., et al. Randomized comparison of different prostaglandin analogues and laminaria tent for preoperative cervical dilation. Contraception 34 237-251 (1986).

Jumblatt, M.M., and Paterson, C.A. Prostaglandin E₂ effects on corneal endothelial cyclic adenosine monophosphate synthesis and cell shape are mediated by a receptor of the EP₂ subtype. Invest Ophthamol Vis Sci 32 360-365 (1991).

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 Ther 271 390-396 (1994).

Toppozada, M., Warda, A., and Ramadan, M. Intramuscular 16-phenoxy PGE₂ ester for pregnancy termination. Prostaglandins 17 461-467 (1979).

Strong, P., Coleman, R.A., and Humphrey, P.P.A. Prostanoid-induced inhibition of lipolysis in rat isolated adipocytes: Probable involvement of EP₃ receptors. Prostaglandins 43 559-566 (1992).

Schaaf, T.K., Bindra, J.S., Eggler, J.F., et al. N-(methanesulfonyl)-16-phenoxyprostaglandincarboxamides: Tissue-selective, uterine stimulants. J Med Chem 24 1353-1359 (1981).

De Vries, G.W., Guarino, P., McLaughlin, A., et al. An EP receptor with a novel pharmacological profile in the T-cell line Jurkat. Br J Pharmacol 115 1231-1234 (1995).

Krishna, U., Gupta, A.N., Ma, H., et al. Randomized comparison of different prostaglandin analogues and laminaria tent for preoperative cervical dilation. Contraception 34 237-251 (1986).

Schillinger, E., Prior, G., Speckenbach, A., et al. Receptor binding in various tissues of PGE₂, and sulprostone, a novel PGE₂-derivative. Prostaglandins 18 293-302 (1979).

Negishi, M., Harazono, A., Sugimoto, Y., et al. TEI-3356, a highly selective agonist for the prostaglandin EP₃ receptor. Prostaglandins 48 275-283 (1994).

Abramovitz, M., Adam, M., Boie, Y., et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta 1483 285-293 (2000).

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Sulprostone is available in the following screening libraries:

• Prostaglandin Screening Library II (96-Well)
• Bio-active Lipid I Screening Library (96-Well)