7054-25-3

• 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：2026-07-16 19:40:38
• 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]。

名称

• 中文名: 葡萄糖酸奎尼丁
• 英文名: quinidine D-gluconate
• 中文别名: 葡萄糖酸奎尼丁 标准品; 喹尼丁葡糖酸盐
• 英文别名: QUINIDINE GLUCONATE; QUINIDINE GLUCONATE //BP; Aficamten Impurity 44; d-gluconicacid,compd.with(9s)-6’-methoxycinchonan-9-ol(1:1); compd.withquinidine(1:1),d-gluconicaci; 6’-methoxy-cinchonan-9-o(9s)-cinchonan-9-omono-d-gluconate(salt); quinidinemono-d-gluconate(salt); QUINIDINEGLUCONATE; QUINIDINE GLUCONATE SALT

物化性质

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

生物活性

• 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:
  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.

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)

安全

• 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)