生物活性 靶点 体外研究 体内研究
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乙氢去甲奎宁

乙氢去甲奎宁,522-60-1,结构式
乙氢去甲奎宁
  • CAS号:522-60-1
  • 英文名:ETHYLHYDROCUPREINE
  • 中文名:乙氢去甲奎宁
  • CBNumber:CB4490364
  • 分子式:C21H28N2O2
  • 分子量:340.46
  • MOL File:522-60-1.mol
乙氢去甲奎宁化学性质
  • 熔点 :123-128° when solvent-free
  • 比旋光度 :D25 -136.2° (alcohol)
  • 沸点 :476.25°C (rough estimate)
  • 密度 :1.1027 (rough estimate)
  • 折射率 :1.6180 (estimate)
  • 储存条件 :2-8°C
安全信息
  • 危险品标志 :Xn
  • 危险类别码 :22
  • WGK Germany :3
  • RTECS号 :MW5950000

乙氢去甲奎宁性质、用途与生产工艺

  • 生物活性 Ethylhydrocupreine (Optochin) 是一种具有抗菌作用的奎宁衍生物,具有抗肺炎链球菌 (S. pneumoniae) 的活性。Ethylhydrocupreine 还具有抗 Plasmodium falciparum 的抗疟活性,IC50 为 25.75 nM。Ethylhydrocupreine 是一种 Gallus gallus 2 受体 (ggTas2r1,ggTas2r2 和 ggTas2r7) 激动剂。
  • 靶点

    S. pneumoniae
    IC50: 25.75 nM ( Plasmodium falciparum )
    ggTas2r1, ggTas2r2 and ggTas2r7

  • 体外研究

    The mutation rate to Ethylhydrocupreine (Optochin) resistance is estimated using fluctuation analysis in three capsulated S. pneumoniae strains ( S. pneumoniae D39 NCTC 7466, S. pneumoniae R6 ATCC BAA-255 and S. pneumoniae ATCC 49619). The exposure to subinhibitory concentrations of penicillin increased the mutation rate (expressed as mutation per cell division) to Ethylhydrocupreine (Optochin) resistance between 2.1- and 3.1-fold for all three strains studied.

  • 体内研究

    The injection of 1 cc. of a 24 hour dextrose blood broth culture of virulent Type I pneumococci into the right pleural cavity of guinea pigs produces acute suppurative pleuritis on both sides associated with suppurative pericarditis. The injection of 1 cc. of 1:500 solutions of Ethylhydrocupreine hydrochloride into each pleural cavity of guinea pigs at varying intervals up to 24 hours after pleural infection has usually shown a marked curative influence. Similar results are observed with dogs.

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