多拉司琼

• 常用名: 多拉司琼
• 英文名: Dolasetron
• CAS号: 115956-12-2
• 分子量: 324.37400
• 密度: 1.37 g/cm3
• 沸点: 535.1ºC at 760 mmHg
• 分子式: C₁₉H₂₀N₂O₃
• 熔点: 278 ºC
• 闪点: 277.4ºC

多拉司琼用途

Dolasetron(MDL-73147)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。

多拉司琼名称

• 中文名: 多拉司琼
• 英文名: (2alpha,6alpha,8alpha,9abeta)-Octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl-1H-indole-3-carboxylate

多拉司琼生物活性

• 描述: Dolasetron(MDL-73147)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.

  [2]. Schwartzberg L, et al. Pooled analysis of phase III clinical studies of palonosetron versus ondansetron, dolasetron, and granisetron in the prevention of chemotherapy-induced nausea and vomiting (CINV). Support Care Cancer. 2014 Feb;22(2):469-77.

多拉司琼物理化学性质

• 密度: 1.37 g/cm3
• 沸点: 535.1ºC at 760 mmHg
• 熔点: 278 ºC
• 分子式: C₁₉H₂₀N₂O₃
• 分子量: 324.37400
• 闪点: 277.4ºC
• 精确质量: 324.14700
• PSA: 62.40000
• LogP: 2.45690
• InChIKey: UKTAZPQNNNJVKR-UDXKHGJESA-N
• SMILES: O=C(OC1CC2CC3CC(C1)N2CC3=O)c1c[nH]c2ccccc12
• 外观性状: 固体;White to Almost white powder to crystaline
• 蒸汽压: 4.08E-10mmHg at 25°C
• 折射率: 1.76
• 储存条件: Refrigerator
• 水溶解性: 可溶
• 分子结构:

  1、 摩尔折射率：88.81

  2、 摩尔体积（cm³/mol）：236.1

  3、 等张比容（90.2K）：671.0

  4、 表面张力（dyne/cm）：65.2

  5、 极化率（10-24cm3）：35.20

多拉司琼安全信息

• 危害码 (欧洲): Xi
• 风险声明 (欧洲): R36/37/38:Irritating to eyes, respiratory system and skin .
• 安全声明 (欧洲): S26:In case of contact with eyes, rinse immediately with plenty of water and seek medical advice . S36:Wear suitable protective clothing .
• WGK德国: 3

多拉司琼制备

环戊烯羧酸乙酯(Ⅰ)，在催化量的四氧化锇存在下，用N-甲基吗啉-N-氧化物氧化为二醇(Ⅱ)。再在过碘酸钠作用下分裂为二醛(Ⅲ)，其水溶液在pH值4时，通过Robinson-Schoepf反应转化为双环化物(Ⅳ)。(Ⅳ)再用硼氢化钠还原为醇(Ⅴ)，和二氢吡喃反应形成四氢呋喃醚(Ⅵ)，以保护形成的羟基。然后转化为三环化物(Ⅶ)，接着在四氟硼银存在下，和酰氯(Ⅷ)反应，酰化得到多拉司琼。

多拉司琼靶点实验

查看更多实验

实验名称：Increase the activity of the Burkholderia fixLJ 2-component system 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Burkholderia multivorans External Id：HMS1625

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：Chemical Probes of Kaposi's Sarcoma Herpes Virus Latent Infection 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：ORF 73 [Human herpesvirus 8 type M] External Id：HMS791

实验名称：Rescue cell viability in cybrid cells with a genetic mutation in complex 1 of the mit... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1315

实验名称：High-throughput screen for inhibitors of the GIV GBA-motif interaction with Galpha-i ... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS1303

实验名称：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

实验名称：Phenotypic Assay to Identify Small Molecules that Upregulate Production of hCFTR in H... 来源：Southern Research Institute 靶标：CFTR External Id：CF Folding

实验名称：MELAS cybrid survival enhancement under low glucose conditions 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：N/A External Id：HMS1419

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多拉司琼英文别名

• Dolasetronum [inn-latin]
• Dolasetron
• (2a,6a,8a,9ab)-1H-Indole-3-carboxylic acid,octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester
• 1H-Indole-3-carboxylic acid,octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester,(2alpha,6alpha,8alpha,9abeta)
• Dolasetronum
• Octahydro-3-oxo-2,6-Methano-2H-quinolizin-8-yl Ester
• Unii-82wi2L7Q6e