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522-60-1

中文名称 乙氢去甲奎宁
CAS 522-60-1
分子式 C21H28N2O2
分子量 340.46
MOL 文件 522-60-1.mol
522-60-1 结构式 522-60-1 结构式

基本信息

中文别名
乙氢去甲奎宁
乙基氢化脱甲奎宁
乙基氢化铜色树碱
乙基氢化铜色金鸡纳碱
英文别名
optochin
numoquin
optoquine
Optochine
Numoquine
Ethylhydrocuprein
ETHYLHYDROCUPREINE
hydrocupreineethylether
Hydrocupureine ethyl ether
6’-ethoxy-hydrocinchonidin

物理化学性质

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
形态neat

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
危险品标志Xn
危险类别码22
WGK Germany3
RTECS号MW5950000

常见问题列表

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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