4,5-Dihydro-N-[4-[[4-(1-methylethoxy)phenyl]carbonyl]phenyl]-1H-imidazol-2-amine

Recently, a series of relatively simple compounds were found to be high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor. CAY10449 is one of the more potent of these. CAY10449 antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a K_i value of about 3 nM. Although CAY10449 was not tested in rats, the related compound CAY10441 shows significant analgesic activity in standard antinociceptive assays.

[1] ROBIN D. CLARK . Erratum to “Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists”[J]. Bioorganic & Medicinal Chemistry Letters, 2004, 14 10: Page 2697. DOI: 10.1016/j.bmcl.2004.02.030