Description
The prostaglandin E
2 (PGE
2) receptor (EP
1) is involved in triggering PGE
2-
mediated pain as well as neuronal survival and growth. SC-
51322 is a selective EP
1 antagonist that inhibits PGE
2 signaling in a guinea pig ileum muscle strip assay with a pA
2 value of 8.1 and demonstrates analgesic activity in a mouse writhing assay with an ED
50 value of 0.9 mg/kg. It is pharmacologically similar to SC-
51089, but does not release hydrazine, a known carcinogen to rats, as does SC-
51089. SC-
51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE
2 with an EC
50 value of 7.75 μM.
References
[1] E. ANN HALLINAN. Aminoacetyl Moiety as a Potential Surrogate for Diacylhydrazine Group of SC-51089, a Potent PGE2 Antagonist, and Its Analogs[J]. Journal of Medicinal Chemistry, 1996, 39 2: 609-613. DOI:
10.1021/jm950454k[2] N FOUDI. Vasorelaxation induced by prostaglandin E2 in human pulmonary vein: role of the EP4 receptor subtype[J]. British Journal of Pharmacology, 2009, 154 8: 1631-1639. DOI:
10.1038/bjp.2008.214
