乙氢去甲奎宁 CAS#: 522-60-1

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乙氢去甲奎宁

生物活性靶点体外研究体内研究

中文名称	乙氢去甲奎宁
中文同义词	乙氢去甲奎宁;乙基氢化铜色金鸡纳碱;乙基氢化铜色树碱;乙基氢化脱甲奎宁;(R)-(6-乙氧基喹啉-4-基)((1S,2S,4S,5R)-5-乙基奎宁-2-基)甲醇;化合物 ETHYLHYDROCUPREINE
英文名称	ETHYLHYDROCUPREINE
英文同义词	optochin;optoquine;ethylhydrocupreine free base*crystalline;Numoquine;Optochine;Ethylhydrocuprein;Hydrocupureine ethyl ether;Cinchonan-9-ol,6'-ethoxy-10,11-dihydro-, (8a,9R)-
CAS号	522-60-1
分子式	C21H28N2O2
分子量	340.46
EINECS号	208-333-5
相关类别	乙氢去甲奎宁;Miscellaneous
Mol文件	522-60-1.mol
结构式

乙氢去甲奎宁 性质

乙氢去甲奎宁 用途与合成方法

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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