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硫酸奎尼丁

硫酸奎尼丁用途

【用途一】
Class IA型抗心律失常药，钾通道阻障剂。

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硫酸奎尼丁名称

[ CAS 号 ]:
6591-63-5

[ 中文名 ]:
硫酸奎尼丁二水合物

[ 英文名 ]:
Quinidine sulfate dihydrate

[中文别名 ]:

[英文别名 ]:

Quinidine Sulfate Dihydrate
EINECS 200-046-3
MFCD00149346

硫酸奎尼丁生物活性

[ 描述 ]:

Quinidine sulfate dihydrate 是一种有效且选择性的细胞色素 P450db (cytochrome P450db) 抑制剂,可在体内抑制苯丙胺的代谢。Quinidine sulfate dihydrate 增强长春新碱 (VCR) 在肿瘤细胞中的细胞毒性,尤其是在 P388 白血病 (P388/VCR) 和人骨髓性白血病的VCR 耐药亚型中。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450

[ 靶点 ]

IC50: cytochrome P450db; amphetamine metabolism[1]

[参考文献]

[1]. David E. Moody, et al. Quinidine Inhibits In Vivo Metabolism of Amphetamine in Rats: Impact upon Correlation between GCIMS and Immunoassay Findings in Rat Urine. ournal of Analytical Toxicology, Vol. 14, September/October 1990

[2]. Tsuruo T, et al. Effects of quinidine and related compounds on cytotoxicity and cellular accumulation of vincristine and adriamycin in drug-resistant tumor cells.Cancer Res. 1984 Oct;44(10):4303-7.

硫酸奎尼丁物理化学性质

[ 沸点 ]:
992.5ºC at 760 mmHg

[ 熔点 ]:
212-214 °C (dec.)(lit.)

[ 分子式 ]:
C₂₀H₂₄N₂O_2.1/₂H₂O₄S_.H₂O

[ 分子量 ]:
782.943

[ 闪点 ]:
554ºC

[ 精确质量 ]:
782.356079

[ PSA ]:
192.62000

[ LogP ]:
6.52160

[ 外观性状 ]:
固体

[ 折射率 ]:
275 ° (C=2, 0.1mol/L HCl)

[ 储存条件 ]:
室温

硫酸奎尼丁MSDS

详细MSDS(安全技术说明书)

硫酸奎尼丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VA5605000

CHEMICAL NAME :: Quinidine, hemisulfate, hydrate

CAS REGISTRY NUMBER :: 6591-63-5

LAST UPDATED :: 198708

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C20-H24-N2-O2.1/2H2-O4-S.H2-O

MOLECULAR WEIGHT :: 391.52

WISWESSER LINE NOTATION :: T66 A B CNTJ A1U1 DYQ- ET66 BNJ HO1 2 &..H2.S-O4 &QH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 59 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - other changes

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: 123,269,1958

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硫酸奎尼丁安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 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) ]:
R22

[ 安全声明 (欧洲) ]:
13-36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
VA5605000

硫酸奎尼丁文献

Comparative study of the effects of antituberculosis drugs and antiretroviral drugs on cytochrome P450 3A4 and P-glycoprotein.

Antimicrob. Agents Chemother. 58(6) , 3168-76, (2014)

Predicting drug-drug interactions (DDIs) related to cytochrome P450 (CYP), such as CYP3A4 and one of the major drug transporters, P-glycoprotein (P-gp), is crucial in the development of future chemoth...

Diurnal variation in P-glycoprotein-mediated transport and cerebrospinal fluid turnover in the brain.

AAPS J. 16(5) , 1029-37, (2014)

Nearly all bodily processes exhibit circadian rhythmicity. As a consequence, the pharmacokinetic and pharmacodynamic properties of a drug may also vary with time of day. The objective of this study wa...

Effects of the inhibition of intestinal P-glycoprotein on aliskiren pharmacokinetics in cynomolgus monkeys.

Biopharm. Drug Dispos. 36(1) , 15-33, (2015)

Aliskiren is a substrate for P-glycoprotein (P-gp) and is metabolized via cytochrome P450 3A4 (CYP3A4). The aim of the present study was to assess whether P-gp influenced the pharmacokinetics of alisk...

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