乙氢去甲奎宁

乙氢去甲奎宁用途

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。

乙氢去甲奎宁名称

[ CAS 号 ]:
522-60-1

[ 中文名 ]:
乙氢去甲奎宁

[ 英文名 ]:
Ethylhydrocupreine

[中文别名 ]:

乙基氢化脱甲奎宁

[英文别名 ]:

Optochine
hydrocupreineethylether
ETHYLHYDROCUPREINE
Hydrocupureine ethyl ether
Numoquine
Ethylhydrocuprein
numoquin
optoquine

乙氢去甲奎宁生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

S. pneumoniae[1] IC50: 25.75 nM (Plasmodium falciparum)[3] ggTas2r1, ggTas2r2 and ggTas2r7[4]

[体外研究]

用波动分析法估计了三株肺炎链球菌(肺炎链球菌D39 NCTC 7466、肺炎链球菌R6-ATCC-BAA-255和肺炎链球菌ATCC 49619)对乙基氢嘌呤(Optochin)耐药的突变率。暴露于亚抑制浓度的青霉素可使所有三种研究菌株的抗乙基氢化半胱氨酸(Optochin)的突变率(以每细胞分裂的突变表示)增加了2.1到3.1倍[2]。

[体内研究]

注射1毫升。在豚鼠右侧胸膜腔中培养24小时的强毒株I型肺炎球菌葡萄糖血培养液,在两侧产生急性化脓性胸膜炎,并伴有化脓性心包炎。注射1毫升。在胸膜感染后的24小时内,以不同的间隔将1:500的乙基氢青霉烯盐酸盐溶液注入豚鼠的每个胸膜腔中,通常显示出显著的疗效。在狗身上观察到类似的结果[1]。

[参考文献]

[1]. J A Kolmer, et al. CHEMOTHERAPEUTIC STUDIES WITH ETHYLHYDROCUPREINE HYDROCHLORIDE IN EXPERIMENTAL PNEUMOCOCCUS PLEURITIS. J Exp Med. 1921 May 31;33(6):693-711.

[2]. Paulo R Cortes, et al. Subinhibitory Concentrations of Penicillin Increase the Mutation Rate to Optochin Resistance in Streptococcus Pneumoniae. J Antimicrob Chemother. 2008 Nov;62(5):973-7.

[3]. Nassira Mahmoudi, et al. Identification of New Antimalarial Drugs by Linear Discriminant Analysis and Topological Virtual Screening. J Antimicrob Chemother. 2006 Mar;57(3):489-97.

[4]. Antonella Di Pizio, et al. Molecular Features Underlying Selectivity in Chicken Bitter Taste Receptors. Front Mol Biosci. 2018 Jan 31;5:6.

乙氢去甲奎宁物理化学性质

[ 密度 ]:
1.18g/cm3

[ 沸点 ]:
508.7ºC at 760mmHg

[ 熔点 ]:
123-128° when solvent-free

[ 分子式 ]:
C₂₁H₂₈N₂O₂

[ 分子量 ]:
340.45900

[ 闪点 ]:
261.5ºC

[ 精确质量 ]:
340.21500

[ PSA ]:
45.59000

[ LogP ]:
3.72520

[ 折射率 ]:
1.618

[ 储存条件 ]:
2-8°C

乙氢去甲奎宁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW5950000

CHEMICAL NAME :: Hydrocupreine, O(sup 6')-ethyl-

CAS REGISTRY NUMBER :: 522-60-1

BEILSTEIN REFERENCE NO. :: 0092227

LAST UPDATED :: 199709

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C21-H28-N2-O2

MOLECULAR WEIGHT :: 340.51

WISWESSER LINE NOTATION :: T66 BNJ HO2 EYQ- DT66 A B CNTJ G2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

REFERENCE :: OPHTAD Ophtalmologica. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.96- 1978- Volume(issue)/page/year: 143,154,1962 ** ACUTE TOXICITY DATA **

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: HBAMAK "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." (Leipzig, Ger. Dem. Rep.) Volume(issue)/page/year: 4,1289,1935

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 24 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: HBAMAK "Abdernalden's Handbuch der Biologischen Arbeitsmethoden." (Leipzig, Ger. Dem. Rep.) Volume(issue)/page/year: 4,1289,1935

乙氢去甲奎宁安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
MW5950000

[ 海关编码 ]:
2933990090

乙氢去甲奎宁海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

乙氢去甲奎宁文献

Identifying mutator phenotypes among fluoroquinolone-resistant strains of Streptococcus pneumoniae using fluctuation analysis.

Antimicrob. Agents Chemother. 51 , 3225-9, (2007)

The occurrence of mutator phenotypes among laboratory-generated and clinical levofloxacin-resistant strains of Streptococcus pneumoniae was determined using fluctuation analysis. The in vitro selectio...

Genotypic identification of presumptive Streptococcus pneumoniae by PCR using four genes highly specific for S. pneumoniae.

J. Med. Microbiol. 55(Pt 6) , 709-14, (2006)

It was previously reported that two oligonucleotide primer sets (spn9802 and spn9828) for discriminating Streptococcus pneumoniae from pneumococcus-like oral streptococcal isolates using PCR had been ...

Possible overestimation of penicillin resistant Streptococcus pneumoniae colonization rates due to misidentification of oropharyngeal streptococci.

Diagn. Microbiol. Infect. Dis. 42(4) , 263-8, (2002)

Standard identification of Streptococcus pneumoniae by optochin and bile solubility testing can lead to ambiguous results for certain isolates. Newer bacteriologic identification techniques (e.g., DNA...

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