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盐酸奎宁

盐酸奎宁用途

盐酸奎宁是一种从金鸡纳树皮中提取的口服活性生物碱,可用于抗疟疾研究。盐酸奎宁是一种钾通道抑制剂,可抑制电压脉冲诱发的WT小鼠Slo3(KCa5.1)通道电流至+100 mV,IC50为169μM[1][2]。

盐酸奎宁名称

[ CAS 号 ]:
60-93-5

[ 中文名 ]:
盐酸奎宁

[ 英文名 ]:
(-)-Quinine dihydrochloride

[中文别名 ]:

奎宁二盐酸盐

[英文别名 ]:

(8α,9R)-6'-Methoxycinchonan-9-ol dihydrochloride
QuinineDihydrochlorideInjection
MFCD00151247
Quinine dihydrochloride
acidquininehydrochloride
UNII:8C3EMH7D9X
QUININE DI HCL
chinindihydrochlorid
quininebimuriate
Quinine dichloride

盐酸奎宁生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 跨膜转运 >> 钾通道

[体外研究]

盐酸奎宁(150μM,30分钟)抑制人肝癌HepG2细胞系中登革热病毒的增殖和细胞抑制作用[1]。盐酸奎宁(37.5-150μM,24小时)以剂量依赖性方式显著降低人肝癌HepG2细胞系中的病毒DENV RNA和蛋白质水平[1]。细胞增殖试验[1]细胞系：人肝癌细胞系(HepG2)浓度：150μM孵育时间：30分钟结果：与未处理相比,抑制DENV病毒复制,产率为19%。以剂量依赖性方式将DENV阳性细胞从23.28%减少到12.05%。

[体内研究]

盐酸奎宁(口服灌胃,12或15 mg/kg,每周,16周)对瑞士白化小鼠的皮肤癌有一定的抑制作用[2]。盐酸奎宁(口服灌胃,10 mg/kg,每日,8周)导致雄性成年白化大鼠睾丸组织抗氧化防御系统(如SOD、CAT和GSH酶活性)降低[3]。动物模型：7-8周(体重24g)的瑞士白化小鼠[2]剂量：12mg/kg,15mg/kg给药：口服灌胃；每周；16周结果：在12mg/kg剂量下,肿瘤大小和重量显著减少,而在15mg/kg更高剂量下,影响很小。

[参考文献]

[1]. Shilu Malakar，et al. Drug repurposing of quinine as antiviral against dengue virus infection. Virus Res. 2018 Aug 15;255:171-178. doi: 10.1016/j.virusres.2018.07.018. Epub 2018 Jul 25.

[2]. Jhanwar, Deepika，et al. Chemoprevention of DMBA induced skin carcinogenesis in swiss albino mice by quinine sulfate.(2016): 2636-2640.

[3]. Ebenezer O Farombi, et al. Quercetin protects against testicular toxicity induced by chronic administration of therapeutic dose of quinine sulfate in rats. J Basic Clin Physiol Pharmacol. 2012 Feb 27;23(1):39-44.

盐酸奎宁物理化学性质

[ 沸点 ]:
495.9ºC at 760 mmHg

[ 熔点 ]:
238-2400C

[ 分子式 ]:
C₂₀H₂₆Cl₂N₂O₂

[ 分子量 ]:
397.339

[ 闪点 ]:
253.7ºC

[ 精确质量 ]:
396.137146

[ PSA ]:
45.59000

[ LogP ]:
4.71510

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
室温，密封，干燥

[ 稳定性 ]:
Stable, but may be light sensitive. Efflorescent. Incompatible with strong oxidizing agents.

盐酸奎宁MSDS

详细MSDS(安全技术说明书)

盐酸奎宁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VA6478000

CHEMICAL NAME :: Quinine, dihydrochloride

CAS REGISTRY NUMBER :: 60-93-5

LAST UPDATED :: 199709

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C20-H24-N2-O2.2Cl-H

MOLECULAR WEIGHT :: 397.38

WISWESSER LINE NOTATION :: T66 BNJ HO1 EYQ- DT66 A B CNTJ A1U1 &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1392 mg/kg

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

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 78 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 660 mg/kg

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

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 86 mg/kg

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

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 641 mg/kg

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

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 199 mg/kg

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

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 57 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Bacteria - Salmonella typhimurium

DOSE/DURATION :: 2800 nmol/plate

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 66,33,1979

盐酸奎宁安全信息

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
1544

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2939200000

盐酸奎宁合成路线

详细合成路线

盐酸奎宁海关

[ 海关编码 ]: 2939200000