SC-19220 is a dibenzoxazepine which acts as a selective antagonist of prostaglandin E₂ (PGE₂) at the EP₁ receptor.^1,2 At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE₂-induced smooth muscle contractions of guinea pig ileum and stomach.^3,4 SC-19220 acts as a PGE₂ antagonist in the EP₁ receptor mediated contraction of guinea pig trachea.⁵ SC-19220 displaces radiolabeled PGE₂ from the cloned human EP₁ receptor with an IC₅₀ of 6.7 µM and exhibits no binding at the human EP₂ receptor.^6,7 It binds very weakly and shows no selectivity for the mouse EP₁ receptor, suggesting species differences between the human and mouse EP₁ receptors.⁸

1 Coleman, R.A., Eglen, R.M., Jones, R.L., et al. Classification of prostanoid receptors IUPHAR receptor compendium. IUPHAR Compendium (1997).

2 Zeng, L., An, S., Goetzl, E.J. Selective regulation of RNK-16 cell matrix metalloproteinases by the EP₄ subtype of prostaglandin E₂ receptor. Biochemistry 35 7159-7164 (1996).

3 Rakovska, A., Milenov, K. Antagonistic effect of SC-19220 on the responses of guinea-pig gastric muscles to prostaglandins E₁, E₂, and F_2α Arch Int Pharmacodyn 268, 59-69 (1984).

4 Sanner, J. Prostaglandin Inhibition with a dibenzoxazepine hydrazide derivative and morphine. Ann N Y Acad Sci 180 396-409 (1971).

5 Coleman, R.A., Kennedy, I. Characterisation of the prostanoid receptors mediating contraction of guinea-pig isolated trachea. Prostaglandins 29 363-375 (1985).

6 Funk, C.D., Furci, L., Fitzgerald, G.A., et al. Cloning and expression of a cDNA for the human prostaglandin E receptor EP₁ subtype. J Biol Chem 268 26767-26772 (1993).

7 Bastien, L., Sawyer, N., Grygorczyk, R., et al. Cloning, functional expression, and characterization of the human prostaglandin E₂ receptor EP₂ subtype. J Biol Chem 269 11873-11877 (1994).

8 Kiriyama, M., Ushikubi, F., Kobayashi, T., et al. Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol 122 217-224 (1997).

Zeng, L., An, S., Goetzl, E.J. Selective regulation of RNK-16 cell matrix metalloproteinases by the EP₄ subtype of prostaglandin E₂ receptor. Biochemistry 35 7159-7164 (1996).

Coleman, R.A., Eglen, R.M., Jones, R.L., et al. Classification of prostanoid receptors IUPHAR receptor compendium. IUPHAR Compendium (1997).

Rakovska, A., Milenov, K. Antagonistic effect of SC-19220 on the responses of guinea-pig gastric muscles to prostaglandins E₁, E₂, and F_2α Arch Int Pharmacodyn 268, 59-69 (1984).

Coleman, R.A., Kennedy, I. Characterisation of the prostanoid receptors mediating contraction of guinea-pig isolated trachea. Prostaglandins 29 363-375 (1985).

Sanner, J. Prostaglandin Inhibition with a dibenzoxazepine hydrazide derivative and morphine. Ann N Y Acad Sci 180 396-409 (1971).

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