Description
BGC 20-1531 is a potent and selective antagonist of the prostaglandin E
2 (PGE
2; ) receptor subtype 4 (EP
4) with K
i values of 11.7, >10,000, and >10,000 nM for EP
4, EP
2, and EP
3, respectively. It is selective for EP
4, exhibiting <50% inhibition at 47 ion channels, cell-surface transporters, enzymes, and nuclear receptors at a concentration of 10 μM. BGC 20-1531 antagonizes PGE
2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP
4 receptors. It also reverses PGE
2-induced vasorelaxation (K
b = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE
2-induced increases in carotid blood flow and decreases in carotid resistance with an ID
50 value of 5 mg/kg in dogs.
Uses
BGC 20-1531 Hydrochloride, is a potent and selective EP4 antagonist, exhibiting <50% inhibition at 47 ion channels, cell-surface transporters, enzymes, and nuclear receptors at a concentration of 10 μM. It also Inhibits PGE2-induced vasodilation of middle cerebral and meningeal arterieshuman middle cerebral and middle meningeal arterial rings.
