BAY-1797 is an antagonist of the purinergic P2X4 receptor (IC50 = 0.211 ?M for the human receptor).1 It is selective for P2X4 over P2X1, P2X3, and P2X7 receptors (IC50s = >50, 8.3, and 10.6 ?M, respectively, for the human receptors), as well as a panel of G protein-coupled receptors (GPCRs), ion channels, kinases, and transporters at 10 ?M. BAY-1797 (50 mg/kg) decreases intraplantar prostaglandin E2 levels and reduces non-evoked pain-related behavior in the dynamic weight bearing test in a mouse model of inflammatory pain induced by complete Freund’s adjuvant (CFA).
1.Werner, S., Mesch, S., Hillig, R.C., et al.Discovery and characterization of the potent and selective P2X4 inhibitor N-[4-(3-chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and structure-guided amelioration of Its CYP3A4 induction profileJ. Med. Chem.62(24)11194-11217(2019)