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奎尼丁

奎尼丁用途

Quinidine是抗心律失常药物,可治疗心律失常,也可用作疟疾的治疗。

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奎尼丁名称

[ CAS 号 ]:
56-54-2

[ 中文名 ]:
奎尼丁

[ 英文名 ]:
Quinidine

[中文别名 ]:

[英文别名 ]:

Conchinin
Chinidin
Cin-quin
(8R,9S)-6'-Methoxycinchonan-9-ol
Coccinine
(9S)-6'-Methoxycinchonan-9-ol
Quinidex
Cinchonan-9-ol, 6'-methoxy-, (9S)-
Quinidine [BAN]
Raclopride

奎尼丁生物活性

[ 描述 ]:

Quinidine是抗心律失常药物,可治疗心律失常,也可用作疟疾的治疗。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 心血管疾病

研究领域 >> 感染

[ 靶点 ]

Parasite[1]

[体外研究]

奎尼丁是一种临床抗心律失常药物,可影响心肌中的离子电流,并且已被证明是多种细胞类型中几种K +通道的有效阻断剂。奎尼丁的浴应用导致Ik峰值幅度的剂量依赖性降低。用于在0mV下阻断Ik的Kd估计为41μM。奎尼丁引起Ik衰变速率的剂量依赖性增加,并且这种效应通过膜去极化增强。奎尼丁还引起稳态失活曲线的5mV超极化移位,并增加从失活中恢复的半衰期。奎尼丁不影响在-30 mV测量的灭活开始[1]。

[体内研究]

硫酸奎尼丁迅速被吸收,口服剂量后60-90分钟血浆峰值浓度达到峰值。其他盐(葡萄糖酸盐,聚半乳糖醛酸盐)吸收更慢,峰浓度更低。奎尼丁约占血浆蛋白质的70-90％。它经历肝脏氧化代谢以形成N-氧化物,3-羟基形式,O-去甲基形式和2'-醌二酮。由于副作用,超过半数开始奎尼丁的患者在治疗的第一年内停止。这些通常包括腹泻,恶心和呕吐,这些不一定与高血浆浓度有关[2]。奎尼丁抑制大鼠苯丙胺的代谢。奎尼丁预处理导致p-羟基苯丙胺在24和48小时的排泄量分别显着降低至载体对照水平的7.2和24.1％,同时苯丙胺排泄量在24至48小时内显着增加至542％。控件[3]。

[动物实验]

大鼠：将三只大鼠置于单独的代谢笼中，自由获取食物和水。 24小时后，收集尿液（0小时）并且大鼠接受以下治疗：（1）不治疗; （2）80mg奎尼丁/ kg（po）1.0mL / kg，和（III）50％乙醇（1.0mL / kg）。两小时后，所有三只大鼠以1.0mL / kg接受单剂量的15mg苯丙胺/ kg（po）。然后在给予奎尼丁后24和48小时收集尿液。该过程重复三次。收集尿液后，测量体积和pH值，并将尿液储存直至分析[3]。

[参考文献]

[1]. Kehl SJ, et al. Quinidine-induced inhibition of the fast transient outward K+ current in rat melanotrophs. Br J Pharmacol. 1991 Jul;103(3):1807-13.

[2]. Roden DM, et al. Class I antiarrhythmic agents: quinidine, procainamide and N-acetylprocainamide, disopyramide.

[3]. Moody DE, et al. Quinidine inhibits in vivo metabolism of amphetamine in rats: impact upon correlation between GC/MS and immunoassay findings in rat urine. J Anal Toxicol. 1990 Sep-Oct;14(5):311-7.

[相关活性小分子]

奎尼丁物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
495.9±40.0 °C at 760 mmHg

[ 熔点 ]:
168-172 °C(lit.)

[ 分子式 ]:
C₂₀H₂₄N₂O₂

[ 分子量 ]:
324.417

[ 闪点 ]:
253.7±27.3 °C

[ 精确质量 ]:
324.183777

[ PSA ]:
45.59000

[ LogP ]:
3.44

[ 外观性状 ]:
白色至淡黄色晶体粉末

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.638

[ 储存条件 ]:
0-10°C;避免加热

[ 水溶解性 ]:
0.05 g/100 mL (20 ºC)

奎尼丁MSDS

详细MSDS(安全技术说明书)

奎尼丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VA4725000

CHEMICAL NAME :: Quinidine

CAS REGISTRY NUMBER :: 56-54-2

LAST UPDATED :: 199707

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C20-H24-N2-O2

MOLECULAR WEIGHT :: 324.46

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

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rabbit

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 137,410,1962 ** ACUTE TOXICITY DATA **

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 263 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 27,589,1977

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 23 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 128,22,1960

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 54(3),32,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 535 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 105,291,1952

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 135 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 137,410,1962

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 205,129,1948

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 53600 ug/kg

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

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 27,1142,1984

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

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

REFERENCE :: 27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,232,1973

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 30 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 226,286,1977

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 67 mg/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 48(5),43,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 650 mg/kg/7W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects

REFERENCE :: ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 51,43,1982 *** REVIEWS *** TOXICOLOGY REVIEW FNSCA6 Forensic Science. (Lausanne, Switzerland) V.1-11, 1972-78. For pub lisher information, see FSINDR. Volume(issue)/page/year: 2,67,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - A1119 No. of Facilities: 43 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 85 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - A1119 No. of Facilities: 44 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 1723 (estimated) No. of Female Employees: 975 (estimated)

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奎尼丁安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

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

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36-S22

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
VA4725000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

奎尼丁合成路线

详细合成路线

奎尼丁上下游产品

奎尼丁上游产品

奎尼丁下游产品

奎尼丁制备

为金鸡纳皮所含生物碱，是奎宁的异构体。可由金鸡纳树皮中提取奎宁、辛可宁、辛可尼丁后，从母液中提取奎宁丁，再用硫酸处理而制得。

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奎尼丁海关

[ 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%

奎尼丁文献

Organic anion transporting polypeptides and organic cation transporter 1 contribute to the cellular uptake of the flavonoid quercetin.

Naunyn Schmiedebergs Arch. Pharmacol. 387(9) , 883-91, (2014)

Flavonoids such as quercetin and kaempferol mediate several health protective effects, e.g., anticancer effects. They are inhibitors of organic anion transporting polypeptides (OATP) and organic catio...

Morphological behaviour and metabolic capacity of cryopreserved human primary hepatocytes cultivated in a perfused multiwell device.

Xenobiotica 45(1) , 29-44, (2014)

1. The quantitative prediction of the pharmacokinetic parameters of a drug from data obtained using human in vitro systems remains a significant challenge i.e. prediction of metabolic clearance in hum...

Utility of cerebrospinal fluid drug concentration as a surrogate for unbound brain concentration in nonhuman primates.

Drug Metab. Pharmacokinet. 29(5) , 419-26, (2014)

In central nervous system drug discovery, cerebrospinal fluid (CSF) drug concentration (C(CSF)) has been widely used as a surrogate for unbound brain concentrations (C(u,brain)). However, previous rod...

更多文献

奎尼丁

奎尼丁用途

奎尼丁名称

奎尼丁生物活性

奎尼丁物理化学性质

奎尼丁MSDS

详细MSDS(安全技术说明书)

奎尼丁毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

奎尼丁安全信息

奎尼丁合成路线

详细合成路线

奎尼丁上下游产品

奎尼丁上游产品

奎尼丁下游产品

奎尼丁制备

奎尼丁海关

奎尼丁文献

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