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ChemicalBook  CAS数据库列表  1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐

1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐

生物活性 靶点 体外研究 体内研究
1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐,154164-30-4,结构式
1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐
  • CAS号:154164-30-4
  • 英文名:YM90Khydrochloride
  • 中文名:1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐
  • CBNumber:CB31074818
  • 分子式:C11H7N5O4.HCl
  • 分子量:0
  • MOL File:154164-30-4.mol
1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐化学性质
  • 储存条件 :Desiccate at RT
  • 溶解度 :Soluble to 10 mM in DMSO with gentle warming
  • 形态 :Powder

1,4-二氢-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮单盐酸盐性质、用途与生产工艺

  • 生物活性 YM90K 是一种有效的选择性的 AMPA 受体拮抗剂，Ki 为 84 nM。YM90K 抑制海藻酸酯 (Ki 为 2.2 μM) 和 NMDA (Ki 为 37 μM) 受体的效力较低，并具有神经保护作用。
  • 靶点

    Ki: 84 nM (AMPA receptor), 2.2 μM (Kainate receptor) and 37 μM (NMDA receptor)

  • 体外研究

    YM90K co-injected with AMPA or kainate into the rat striatum protect cholinergic neurons against AMPA- or kainate-induced neurotoxicity.

  • 体内研究

    YM90K shows potent suppressive activity against audiogenic seizure in DBA/2 mice; ED 50 values of YM90K against tonic seizure is 2.54 mg/kg (i.p.). The duration of the anticonvulsant effects of YM90K is 30 min.
    In a global ischemia model, YM90K (15 mg/kg i.p.) significantly prevents the delayed neuronal death in the hippocampal CA1 region in Mongolian gerbils when administered 1 h after 5-min ischemia. The therapeutic time window for the neuroprotective effect of YM90K (30 mg/kg i.p.) is 6 h.
    In a focal ischemia model, YM90K (30 mg/kg i.v. bolus+10 mg/kg/h for 4 h) reduces the volume of ischemic damage in the cerebral cortex in F344 rats.

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