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.
1 Clark, R.D., Jahangir, A., Severance, D., et al. Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg Medicinal Chem Letters 14 1053-1056 (2004).
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