439288-66-1

The effects of prostaglandin E₂ (PGE₂) are transduced by at least four distinct receptors designated EP₁, EP₂, EP₃, and EP₄. GW 627368X is a potent and selective competitive antagonist of the EP₄ receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP₄ and TP receptors with K_i values of 100 nM and 158 nM, respectively. Affinity for all other human prostanoid receptors is >5.0 μM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 μM.

GW 627368 is a selective EP4 receptor competitive antagonist.

EP

[1] RICHARD J WILSON. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist[J]. British Journal of Pharmacology, 2009, 148 3: 326-339. DOI: 10.1038/sj.bjp.0706726