生物活性 靶点 体外研究 体内研究
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2'MEO6MF

2'MEO6MF,89112-85-6,结构式
2'MEO6MF
  • CAS号:89112-85-6
  • 英文名:2-(2-METHOXYPHENYL)-6-METHYL-4H-1-BENZOPYRAN-4-ONE
  • 中文名:2'MEO6MF
  • CBNumber:CB92748271
  • 分子式:C17H14O3
  • 分子量:266.29
  • MOL File:89112-85-6.mol

2'MEO6MF性质、用途与生产工艺

  • 生物活性 2'MeO6MF 是一种可透过血脑屏障的 α2β1γ2L 和所有含 α1 的 GABAA 受体的正变构调节剂。2'MeO6MF 也可以直接激活 α2β2/3 和 α2β2/3γ2L GABAA 受体。2'MeO6MF 具有抗焦虑和镇静作用。2'MeO6MF 可提供神经保护作用并改善功能恢复,还可抑制中风诱发的炎症反应。
  • 靶点

    GABA A receptor

  • 体外研究

    2'MeO6MF (100-300 µM; 60 min) weakly displaces [ 3 H]-flunitrazepam binding to rat brain synaptosomal membranes by 5-10%. 2'MeO6MF enhances [ 3 H]-muscimol binding to rat brain synaptic membranes in a concentration-dependent manner yielding a mean E max of 219.8% and apparent EC 50 =20.8 nM.
    2'MeO6MF (1-300 µM) enhances the response elicited by a low concentration of GABA in a concentration-dependent manner at recombinant α1β2γ2L GABA A receptors expressed in XenopusM oocytes. 2'MeO6MF enhances the response elicited by GABA at recombinant α1β1,3γ2L and α1β2 GABA A receptors without any direct activation.
    2'MeO6MF (1-10 µM; 60 min) increases tonic inhibitory currents in a concentration-dependent manner in granule cells.
    2'MeO6MF (100-1000 µM; 6.5 h) inhibits the LPS-induced increase of NFkB activity in RAWblue TM macrophage cells.

  • 体内研究

    2'MeO6MF (1-100 mg/kg; i.p.) displays anxiolytic-like effects in the elevated plus maze and light/dark tests. 2'MeO6MF induces sedative effects at higher doses in the holeboard, actimeter and barbiturate-induced sleep time tests.
    2'MeO6MF (30 mg/kg; i.p.) increases tonic currents in layer 2/3 pyramidal neurons of mice after stroke.
    2'MeO6MF (0.1-30 mg/kg; i.p.) is neuroprotective and enhances functional recovery after focal cerebral ischaemia in mice.

    Animal Model: Male Balb-c mice (8-10 weeks, 25-35 g)
    Dosage: 1, 10, 30, 100 mg/kg
    Administration: I.p.
    Result: No overt acute toxicity was observed.
    Exerted anxiolytic effects at low doses and sedative effects at high doses without myorelaxant effects.
2'MEO6MF上下游产品信息
上游原料
下游产品
2'MEO6MF生产厂家
  • 公司名称:TargetMol中国(陶术生物)
  • 联系电话: 4008200310
  • 电子邮件:marketing@tsbiochem.com
  • 国家:中国
  • 产品数:24017
  • 优势度:58
  • 公司名称:TargetMol Chemicals Inc.
  • 联系电话:+1-781-999-5354
  • 电子邮件:support@targetmol.com
  • 国家:美国
  • 产品数:19973
  • 优势度:58