Description
The effects of prostaglandin E
2 (PGE
2) are transduced by at least four distinct receptors designated EP
1, EP
2, EP
3, and EP
4. GW 627368X is a potent and selective competitive antagonist of the EP
4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP
4 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.
