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210245-80-0

中文名称 YM 872
英文名称 ZONAMPANEL
CAS 210245-80-0
分子式 C13H9N5O6
分子量 331.24
MOL 文件 210245-80-0.mol
210245-80-0 结构式 210245-80-0 结构式

基本信息

中文别名
唑南帕奈
英文别名
ZONAMPANEL
Zonampanel (YM 872)
7-(1H-Imidazol-1-yl)-6-nitro-2,3-dioxo-3,4-dihydro-1(2H)-quinoxalineacetic acid
1(2H)-Quinoxalineacetic acid, 3,4-dihydro-7-(1H-imidazol-1-yl)-6-nitro-2,3-dioxo-
1(2H)-Quinoxalineacetic acid, 3,4-dihydro-7-(1H-imidazol-1-yl)-6-nitro-2,3-dihydro-
(2,3-Dioxo-7-(1H-imidazol-1-yl)-6-nitro-1,2,3,4-tetrahydro-1-quinoxalinyl)acetic acid monohydrate

物理化学性质

密度1.82±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)3.20±0.10(Predicted)
形态Solid
颜色Yellow to brown

常见问题列表

生物活性
Zonampanel (YM 872) 是一种选择性的 AMPA 受体拮抗剂。
体外研究

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].

体内研究

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

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