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葡萄糖酸奎尼丁

葡萄糖酸奎尼丁用途

奎宁是一种抗心律失常剂。奎宁是一种有效的口服活性选择性细胞色素P450db抑制剂。奎宁也是一种钾通道阻滞剂,IC50为19.9μM。奎宁可用于疟疾研究[1][2][3]。

葡萄糖酸奎尼丁名称

[ CAS 号 ]:
7054-25-3

[ 中文名 ]:
葡萄糖酸奎尼丁

[ 英文名 ]:
quinidine gluconate

[英文别名 ]:

quinidine gluconate

葡萄糖酸奎尼丁生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 心血管疾病

研究领域 >> 感染

信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450

信号通路 >> 跨膜转运 >> 钾通道

[体外研究]

奎尼丁是一种影响心肌离子电流的抗心律失常药物,也被证明是多种细胞类型中几类钾通道的有效阻断剂[1]。奎尼丁浴应用导致Ik峰值幅度的剂量依赖性降低。在0 mV时阻断Ik的Kd估计为41μM[1]。奎尼丁引起Ik衰减速率的剂量依赖性增加,这种效应通过膜去极化而增强。奎尼丁还会引起稳态失活曲线的5 mV超极化偏移,并增加失活恢复的半衰期。奎尼丁不影响在-30 mV时测得的失活开始[1]。

[体内研究]

硫酸奎尼丁被迅速吸收,口服后60-90分钟达到峰值血浆浓度。其他盐(葡萄糖酸盐、聚半乳糖醛酸盐)吸收较慢,峰值浓度较低[2]。奎尼丁约70-90%与血浆蛋白质结合。它经历肝脏氧化代谢以形成N-氧化物、3-羟基形式、O-脱甲基形式和2’-奎尼酮[2]。奎尼丁抑制大鼠体内苯丙胺的代谢。奎尼丁预处理导致对羟基苯丙胺在24小时和48小时的排泄量分别显著减少至溶媒对照水平的7.2%和24.1%,同时苯丙胺的排泄量在24小时到48小时之间显著增加至对照水平的542%[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.

葡萄糖酸奎尼丁物理化学性质

[ 熔点 ]:
175-176ºC

[ 分子式 ]:
C₂₆H₃₆N₂O₉

[ 分子量 ]:
520.57200

[ 精确质量 ]:
520.24200

[ PSA ]:
184.04000

葡萄糖酸奎尼丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LZ5250000

CAS REGISTRY NUMBER :: 7054-25-3

LAST UPDATED :: 199506

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C20-H24-N2-O2.C6-H12-O7

MOLECULAR WEIGHT :: 520.64

WISWESSER LINE NOTATION :: T66 BNJ HO1 EYQ- DT66 A B CNTJ A1U1 &QVYQYQYQYQ1Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7609 mg/kg/78W-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, allergic (after systemic exposure)

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 145,446,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 337 mg/kg/17D-I

TOXIC EFFECTS :: Blood - changes in cell count (unspecified) Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 77,345,1984

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 23,288,1972 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 83945 No. of Facilities: 33 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 66 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 83945 No. of Facilities: 63 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 9094 (estimated) No. of Female Employees: 8028 (estimated)

葡萄糖酸奎尼丁安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302 + H312 + H332

[ 警示性声明 ]:
P261-P280-P301 + P312 + P330

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

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
20/21/22-36/37/38

[ 安全声明 (欧洲) ]:
36-26

[ 危险品运输编码 ]:
UN 1544

[ RTECS号 ]:
LZ5250000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

葡萄糖酸奎尼丁文献

Disposition of 3-hydroxyquinidine in patients receiving initial intravenous quinidine gluconate for electrophysiology testing of ventricular tachycardia.

DICP 23(5) , 375-8, (1989)

The formation rate constant and elimination rate constant for 3-hydroxyquinidine were determined in eight patients with ventricular tachycardia. These two parameters (mean +/- SD) were found to be 0.7...

Quinidine-induced rheumatic syndromes.

Semin. Arthritis Rheum. 24(5) , 315-22, (1995)

Quinidine is a commonly used antiarrhythmic agent that is rarely associated with rheumatologic toxicity. However, quinidine-induced lupus, antinuclear antibody negative lupus-like syndrome, polymyalgi...

Transfusion-transmitted malaria in a kidney transplant recipient. How safe is our blood transfusion?

Saudi Med. J. 29(2) , 293-5, (2008)

A 51-year-old male patient with living, unrelated kidney transplantation in Iran in June 2001, developed Plasmodium falciparum P. falciparum infection. He was maintained on cyclosporine A, mycophenola...

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