Chemical Name:N-[[4'-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethy
l)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-
2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide
Biological Activity:
EP4 receptor antagonist that is
selective over all other members of the prostanoid receptor family (Ki
values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human
EP4, TP, EP3, DP, FP, IP, EP1 and EP2
receptors respectively). Suppresses PGE2-induced bone formation in
rats and prevents the nociceptive response induced by misoprostol in
formalin-injected mice.
Machwateet al
(2001) Prostaglandin receptor EP4 mediates the bone anabolic effects
of PGE2. Mol.Pharmacol. 60 36. Olivaet al
(2006) Role of periaqueductal grey prostaglandin receptors in formalin-induced
hyperalgesia. Eur.J.Pharmacol. 530 40. Balzaryet al
(2006) Lipopolysaccharide induces epithelium- and prostaglandin E2-dependent
relaxation of mouse isolated trachea through activation of cyclooxygenase
(COX)-1 and COX-2. J.Pharmacol.Exp.Ther. 317 806.
