115956-13-3

• 常用中文名：甲磺酸多拉司琼
• 常用英文名：Dolasetron (Mesylate)
• CAS号：115956-13-3
• 分子式：C₂₀H₂₄N₂O₆S
• 分子量：420.48
• 相关类别： 原料药 消化系统用药 止吐催吐药
• 发布时间：2018-03-03 08:00:00
• 更新时间：2024-01-02 18:28:11
• Dolasetron(MDL-73147)甲磺酸盐是5-HT3受体拮抗剂,用于只治疗化疗引起的恶心和呕吐症状。

名称

• 中文名: 甲磺酸多拉司琼
• 英文名: Dolasetron mesylate hydrate
• 中文别名: 多拉司琼甲磺酸盐
• 英文别名: (1r,3R,5r,7S)-10-Oxo-8-azatricyclo[5.3.1.0]undec-5-yl 1H-indole-3-carboxylate methanesulfonate hydrate (1:1:1); MFCD01718979; Dolasetron mesylate; (3R,5r,7S)-10-Oxo-8-azatricyclo[5.3.1.0]undec-5-yl 1H-indole-3-carboxylate methanesulfonate hydrate (1:1:1); 1H-Indole-3-carboxylic acid, (6R,9aS)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, methanesulfonate, hydrate (1:1:1); EINECS 214-599-3; Dolasetron (Mesylate)

物化性质

• 沸点: 535.1ºC at 760 mmHg
• 分子式: C₂₀H₂₄N₂O₆S
• 分子量: 420.48
• 闪点: 277.4ºC
• PSA: 134.38000
• LogP: 2.97740
• 外观性状: 白色粉末
• 蒸汽压: 1.65E-22mmHg at 25°C
• 储存条件: 2-8°C

生物活性

• 描述: Dolasetron(MDL-73147)甲磺酸盐是5-HT3受体拮抗剂,用于只治疗化疗引起的恶心和呕吐症状。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
  研究领域 >> 其他
• 参考文献:

  [1]. Faria C, et al. Outcomes Associated with 5-HT3-RA Therapy Selection in Patients with Chemotherapy-Induced Nausea and Vomiting: A Retrospective Claims Analysis. Am Health Drug Benefits. 2014 Jan;7(1):50-8.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : NL6015300 CHEMICAL NAME : 1H-Indole-3-carboxylic acid, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, (2-alpha,6-alpha,8-alpha,9a-beta)-, monomethanesulfonate, monohydrate CAS REGISTRY NUMBER : 115956-13-3 LAST UPDATED : 199801 DATA ITEMS CITED : 4 MOLECULAR FORMULA : C19-H20-N2-O3.C-H4-O3-S.H2-O MOLECULAR WEIGHT : 438.54 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 2400 ug/kg TOXIC EFFECTS : Behavioral - headache Gastrointestinal - decreased motility or constipation Gastrointestinal - other changes REFERENCE : BDDID8 Biopharmaceutics & Drug Disposition. (John Wiley & Sons, Baffins Lane, Chichester, W. Sussex PO19 1UD, UK) V.1- 1979- Volume(issue)/page/year: 18,361,1997 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - woman DOSE/DURATION : 2400 ug/kg/10M-C TOXIC EFFECTS : Behavioral - hallucinations, distorted perceptions Behavioral - headache REFERENCE : BDDID8 Biopharmaceutics & Drug Disposition. (John Wiley & Sons, Baffins Lane, Chichester, W. Sussex PO19 1UD, UK) V.1- 1979- Volume(issue)/page/year: 18,361,1997 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 545 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 18,506,1993 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 165 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 18,506,1993

安全

• 风险声明 (欧洲): R20/21/22