Recently, a series of relatively simple compounds were found to be high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor.1 CAY10441 is one of the more potent of these. CAY10441 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 Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays.1
1
Clark, R.D., Jahangir, A., Severance, D., et al. Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg Med Chem Lett141053-1056(2004).
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SMILES
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CC(C)Oc1ccc(cc1)Cc1ccc(cc1)NC1=NCCN1
Background Reading
Clark, R.D., Jahangir, A., Severance, D., et al. Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg Med Chem Lett141053-1056(2004).
CAY10441 is available in the following screening
library: