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
- 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
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。
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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.
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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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