RO1138452 is one of the more potent high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor. RO1138452 antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, RO1138452 inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, RO1138452 shows significant analgesic activity in standard antinociceptive assays.