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利诺吡啶

利诺吡啶,105431-72-9,结构式
利诺吡啶
  • CAS号:105431-72-9
  • 英文名:1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE
  • 中文名:利诺吡啶
  • CBNumber:CB6283722
  • 分子式:C26H21N3O
  • 分子量:391.46
  • MOL File:105431-72-9.mol
利诺吡啶化学性质
  • 熔点 :186-186.5 °C
  • 沸点 :655.9±50.0 °C(Predicted)
  • 密度 :1?+-.0.06 g/cm3(Predicted)
  • 储存条件 :Desiccate at RT
  • 溶解度 :DMSO: >10mg/mL
  • 酸度系数(pKa) :6.01±0.10(Predicted)
  • 形态 :A crystalline solid
  • 颜色 :white to off-white
安全信息
  • WGK Germany :3

利诺吡啶性质、用途与生产工艺

  • 生物活性 Linopirdine (DuP 996) 是一种具有口服活性的,选择性 M 型 K+ 电流 (IM;Kv7;KCNQ Channels) 抑制剂,IC50 为 2.4 μM。Linopirdine 是 TRPV1 激活剂。Linopirdine 是一种公认的认知增强药物,可增加大鼠脑组织中乙酰胆碱的释放。
  • 靶点

    IC50: 2.4 μM (M-type K + current)

  • 体外研究

    Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC 50 of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K + leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na + /K + inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC 50 >300 μM).
    Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1).

  • 体内研究

    Linopirdine (DuP 996; i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently increases MAP by up to 15%.

    Animal Model: Male Sprague-Dawley rats (300-350 g)
    Dosage: 0.1, 0.5, 1, 3, 6 mg/kg
    Administration: 5 intravenous bolus injections of increasing doses
    Result: Transiently and dose-dependently increases MAP by up to 15%.
利诺吡啶上下游产品信息
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利诺吡啶生产厂家
  • 公司名称:Labinova AB
  • 联系电话:--
  • 电子邮件:info@labinova.se
  • 国家:欧洲
  • 产品数:281
  • 优势度:64
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