Molecular Formula | C13H9N5O6 |
Molar Mass | 331.24 |
Density | 1.82±0.1 g/cm3(Predicted) |
pKa | 3.20±0.10(Predicted) |
In vitro study | Zonampanel inhibits the human MRP4-mediated transport of [ 3 H]oestradiol 17-D-glucuronide in a concentration-dependent manner. In contrast, Zonampanel (up to 1000 mM) does not inhibit the human MRP2- or BCRP-mediated transport of [ 3 H]oestradiol 17-D-glucuronide or [ 3 H]methotrexate. Zonampanel inhibits the uptake of typical substrates by Oat1, Oat2, and Oat3 with inhibition constant (K i ) values of 7.02 to 10.4 μM. A time- and saturable concentration-dependent increase in [ 14 C]Zonampanel uptake is observed in these cells [K m values: 13.4 to 53.6 μM]. |
In vivo study | In in vivo experiments, probenecid and cimetidine decrease intrinsic clearance for both the renal secretion and biliary excretion of Zonampanel. |
biological activity | Zonampanel (YM 872) is a selective AMPA receptor antagonist. |