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Zonampanel

CAS No. : 210245-80-0

MCE 国际站：Zonampanel

产品活性：Zonampanel (YM 872) 是一种选择性的 AMPA 受体拮抗剂。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

In Vitro: 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 (K_i) values of 7.02 to 10.4 μM. A time- and saturable concentration-dependent increase in [¹⁴C]Zonampanel uptake is observed in these cells [K_m values: 13.4 to 53.6 μM].

In Vivo: In in vivo experiments, probenecid and cimetidine decrease intrinsic clearance for both the renal secretion and biliary excretion of Zonampanel.

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