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Tropisetron HCl

盐酸托烷司琼,ICS 205-930,ICS205-930

Tropisetron是一种选择性5-HT3受体拮抗剂和α7-烟碱受体激动剂，作用于5-HT3受体，IC50为70.1±0.9 nM。

目录号
EY0816
EY0816
EY0816
EY0816
纯度
99.39%
99.39%
99.39%
99.39%
规格
5 mg
10 mg
50 mg
100 mg
原价
345
590
925
1150
售价
345
590
925
1150
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    Tropisetron HCl is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Macor JE, et al. Bioorg Med Chem Lett,?001, 11(3), 319-321.
    [2] Seynaeve et al (1991) 5-HT3 receptor antagonists, a new approach in emesis: a review of ondansetron, granisetron and tropisetron. Anticancer Drugs 2 343.
    [3] Mhatre et al (2004) 5-HT3 antagonist ICS 205-930 enhances naltrexone's effects on ethanol intake. Eur.J.Pharmacol. 491 149.
    [4] Papke et al (2004) Activity of α7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes. Bioorg.Med.Chem.Lett. 14 1849.
    [5] Middlemiss and Tricklebank (1992) Centrally active 5-HT receptor agonists and antagonists. Neurosci.Biobehav.Rev. 16 75.

    分子式
    C17H20N2O2.HCl    		 分子量
    320.81    		 CAS号
    105826-92-4     		储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    50 mM    		 Water
    100 mM    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01895010 Nausea|Vomiting|Metastatic Liver Cancer Device: acupoint electric stimulation|Drug: tropisetron Fudan University Phase 2 2013-06-01 2013-07-09
    NCT00435370 Smoking Cessation|Schizophrenia Drug: Tropisetron|Drug: Placebo|Drug: Risperidone Baylor College of Medicine|National Institute of Mental Health (NIMH) Phase 3 2006-11-01 2017-02-04
    NCT00487110 Pain Drug: Tropisetron|Drug: paracetamol University Hospital, Clermont-Ferrand Phase 4 2008-06-01 2010-03-26
    NCT00889499 Pain|Chronic Disease Drug: Tropisetron 2 mg|Drug: Tropisetron 5mg|Drug: Placebo University Hospital Inselspital, Berne Phase 2 2009-03-01 2011-03-23
    NCT01304953 Pain, Postoperative Drug: Group P+P|Drug: Group P+T|Drug: Group S+P|Drug: Group S+T Huazhong University of Science and Technology Phase 4 2010-01-01 2011-02-25
    NCT02096835 Postoperative Nausea and Vomiting Device: Transcutaneous electrical acupoint stimulation|Device: Sham transcutaneous electrical acupoint stimulation|Drug: Tropisetron|Drug: Dexamethasone Huashan Hospital 2014-01-01 2015-10-09
    NCT00970450 Analgesia Drug: Paracetamol|Drug: Tropisetron|Drug: Placebo University Hospital, Basel, Switzerland 2009-11-01 2013-01-28
    NCT02909478 Chemotherapy-induced Nausea and Vomiting|Colorectal Cancer Drug: Aprepitant+Tropisetron|Drug: Dexamethasone+Tropisetron Sun Yat-sen University Phase 3 2016-12-01 2016-09-19
    NCT01226381 Healthy Volunteers Drug: Von Frey electronic University Hospital, Clermont-Ferrand Phase 1 2010-07-01 2012-02-02
    NCT02576327 Vomiting Drug: Tropisetron|Drug: Dexamethasone|Drug: Aprepitant Jun Zhu|Peking University Phase 4 2015-10-01 2016-12-28
    NCT02478047 Chemotherapy-induced Nausea and Vomiting Drug: only antiemetic (Ramosetron, Tropisetron and dexamethasone)|Other: Matching points ST36+CV12 plus antiemetic drug|Other: Matching points PC6+CV12 plus antiemetic drug|Other: Matching points CV13+CV12 plus antiemetic drug Tianjin University of Traditional Chinese Medicine|National Basic Research Program of China 2015-06-01 2015-06-22
    NCT01843868 Lymphoma, Non-Hodgkin Drug: Standard anti-emetics in conjunction with R-CHOP Australasian Leukaemia and Lymphoma Group|Merck Sharp & Dohme (Australia) Pty Limited 2013-05-01 2013-04-28
    NCT01298193 Breast Cancer Drug: Aprepitant Spanish Breast Cancer Research Group|Merck Sharp & Dohme Corp. Phase 4 2011-05-01 2015-05-18
    NCT01367808 Pharmacokinetics and Pharmacodynamics of Sublingual Buprenorphine Drug: Placebo|Drug: vorikonazole|Drug: posakonazole Turku University Hospital Phase 1 2011-02-01 2011-06-06
    NCT01466803 Healthy Drug: Placebo|Drug: Vorikonazole Turku University Hospital Phase 1 2011-10-01 2013-04-27
    NCT00003817 Nausea and Vomiting|Unspecified Adult Solid Tumor, Protocol Specific Drug: dolasetron mesylate|Drug: granisetron hydrochloride|Drug: ondansetron|Drug: tropisetron|Procedure: quality-of-life assessment Gary Morrow|National Cancer Institute (NCI)|University of Rochester Phase 2 1999-10-01 2015-10-13
    NCT03061396 Electro-acupuncture|Chemotherapy-induced Nausea and Vomiting Other: Matching points PC6+CV12|Other: Single points PC6 Tianjin University of Traditional Chinese Medicine|National Basic Research Program of China|West China Hospital|Tianjin Medical University Cancer Institute and Hospital|Gansu Provincial Cancer Hospital|Henan Provincial Cancer Hospital 2017-03-10 2017-03-01
    NCT01594749 Chemotherapy-Induced Nausea and Vomiting (CINV) Drug: Fosaprepitant dimeglumine|Drug: Fosaprepitant Placebo|Drug: Dexamethasone|Drug: Ondansetron|Drug: Dexamethasone Placebo|Drug: Ondansetron Placebo|Drug: Rescue Therapy Merck Sharp & Dohme Corp. Phase 3 2012-09-01 2017-02-17
    NCT01101529 Nausea|Vomiting Drug: Aprepitant (Emend)|Drug: Placebo Uppsala University Hospital Phase 2 2010-05-01 2012-12-12
    NCT01636947 Nausea|Vomiting Drug: Aprepitant|Drug: Aprepitant Placebo|Drug: Ondansetron|Drug: Dexamethasone|Drug: Ondansetron Placebo|Drug: Rescue Therapy (granisetron, dolasetron, tropisetron or ondansetron; metoclopramide or alizapride). Merck Sharp & Dohme Corp. Phase 4 2012-12-01 2016-12-16

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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