氢溴化奎宁

氢溴化奎宁用途

氢溴酸奎尼丁是一种抗心律失常剂。奎尼丁是一种有效的口服活性选择性细胞色素P450db抑制剂。氢溴酸奎尼丁也是一种钾通道阻滞剂,IC50为19.9μM。氢溴酸奎尼丁可用于疟疾研究[1][2][3]。
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氢溴化奎宁名称

[ CAS 号 ]:
549-49-5

[ 中文名 ]:
氢溴化奎宁

[ 英文名 ]:
quinine hydrobromide

[英文别名 ]:

氢溴化奎宁生物活性

[ 描述 ]:

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

[ 相关类别 ]:

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]

氢溴酸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]。氢溴酸奎尼丁浴应用导致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]。氢溴酸奎尼丁引起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。氢溴酸奎尼丁不影响在-30 mV时测得的失活开始[1]。

[体内研究]

氢溴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]。氢溴酸奎尼丁约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]。氢溴酸奎尼丁抑制大鼠体内苯丙胺的代谢。氢溴酸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.

氢溴化奎宁物理化学性质

[ 密度 ]:
1.21g/cm3

[ 沸点 ]:
495.9ºC at 760mmHg

[ 熔点 ]:
81-82ºC

[ 分子式 ]:
C20H25BrN2O2

[ 分子量 ]:
405.32900

[ 闪点 ]:
253.7ºC

[ 精确质量 ]:
404.11000

[ PSA ]:
45.59000

[ LogP ]:
4.06920

氢溴化奎宁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VA7650000
CHEMICAL NAME :
Quinine, monohydrobromide
CAS REGISTRY NUMBER :
549-49-5
LAST UPDATED :
199709
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C20-H24-N2-O2.Br-H

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
750 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
250 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Bird - pigeon
DOSE/DURATION :
6 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Bird - pigeon
DOSE/DURATION :
1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Amphibian - frog
DOSE/DURATION :
30 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Amphibian - frog
DOSE/DURATION :
18 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FDWU** "Ueber die Wirkung Verschiedener Gifte Auf Vogel, Dissertation," Forchheimer, L., Pharmakologischen Institut der Universitat Wurzburg, Fed. Rep. Ger., 1931 Volume(issue)/page/year: -,-,1931
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氢溴化奎宁安全信息

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
20/21/22-36/37/38-42/43

[ 危险品运输编码 ]:
UN 1544

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
29392000

氢溴化奎宁海关

[ 海关编码 ]: 29392000

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