产品
编 号:F270154
分子式:C13H9N5O6
分子量:331.24
产品类型
结构图
CAS No: 210245-80-0
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产品详情
生物活性:
Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
体内研究:
In in vivo experiments, probenecid and cimetidine decrease intrinsic clearance for both the renal secretion and biliary excretion of Zonampanel.
体外研究:
Zonampanel inhibits the human MRP4-mediated transport of [3H]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 [3H]oestradiol 17-D-glucuronide or [3H]methotrexate. Zonampanel inhibits the uptake of typical substrates by Oat1, Oat2, and Oat3 with inhibition constant (Ki) values of 7.02 to 10.4 μM. A time- and saturable concentration-dependent increase in [14C]Zonampanel uptake is observed in these cells [Km values: 13.4 to 53.6 μM].