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7054-25-3生产厂家

7054-25-3价格

7054-25-3

7054-25-3结构式
7054-25-3结构式
  • 常用中文名:葡萄糖酸奎尼丁
  • 常用英文名:quinidine gluconate
  • CAS号:7054-25-3
  • 分子式:C26H36N2O9
  • 分子量:520.57200
  • 相关类别: 原料药 循环系统用药 抗心律失常药
  • 发布时间:2018-02-22 08:00:00
  • 更新时间:2024-01-02 10:16:03
  • 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]。

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中文名 葡萄糖酸奎尼丁
英文名 quinidine D-gluconate
英文别名 quinidine gluconate
描述 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]。
相关类别
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.

熔点 175-176ºC
分子式 C26H36N2O9
分子量 520.57200
精确质量 520.24200
PSA 184.04000

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)

符号 GHS07
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)