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Donepezil HCl

盐酸多奈哌齐,E 2020,Aricept

Donepezil Hydrochloride是非竞争性的AChE抑制剂,能穿过血脑屏障,增加皮质中的乙酰胆碱水平。

目录号
EY1337
EY1337
EY1337
纯度
99.64%
99.64%
99.64%
规格
50 mg
100 mg
200 mg
原价
540
820
1100
售价
540
820
1100
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    18 μM/kg 腹腔注射或口服给药

  • 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 AKm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] Ogura H, et al. Methods Find Exp Clin Pharmacol. 2000, 22(8), 609-613.
    [2] Shintani, E.Y., et al. 1997. Am J Health Syst Pharm. 54: 2805-2810.
    [3] Bryson, H.M. and Benfield, P. 1997. Drugs Aging. 10: 234-240.
    [4] Kryger et al (1999) Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs. Structure 7 297.
    [5] Sugimoto et al (2000) Donepezil hydrochloride (E2020) and other acetylcholinesterase inhibitors. Curr.Med.Chem. 7 303.

    分子式
    C24H29NO3.HCl
    分子量
    415.95
    CAS号
    120011-70-3
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    1 mg/mL
    Water
    100 mM
    Ethanol
    2 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
    NCT00477659 Alzheimer's Disease Drug: donepezil HCl (Aricept) Eisai Inc.|Pfizer Phase 4 2007-07-01 2009-05-06
    NCT01063556 End-Stage Renal Disease Drug: donepezil HCl|Drug: donepezil HCl Eisai Co., Ltd.|Eisai Inc. Phase 4 2010-02-01 2013-05-13
    NCT02097056 Alzheimer's Disease Drug: Donepezil HCL Eisai Korea Inc.|Eisai Inc. Phase 4 2014-02-01 2016-05-20
    NCT00457769 Stroke|Vascular Dementia|Memory Deficits Drug: Donepezil|Drug: Donepezil Kessler Foundation|Pfizer Phase 1 2007-05-01 2016-02-22
    NCT02064920 Alzheimer's Disease Drug: Placebo|Drug: Donepezil|Drug: Donepezil Merck Sharp & Dohme Corp. Phase 2 2014-04-01 2016-07-24
    NCT00465283 Schizophrenia|Schizoaffective Disorder|Schizophreniform Disorder Drug: Donepezil BeerYaakov Mental Health Center Phase 4 2007-05-01 2009-01-26
    NCT02787746 Alzheimer's Disease Drug: Donepezil Beijing Friendship Hospital Phase 4 2016-05-01 2016-05-26
    NCT01014858 Parkinson's Disease Drug: Donepezil Newcastle-upon-Tyne Hospitals NHS Trust|University of Newcastle Upon-Tyne|University of Cambridge|University of Manchester|University of Birmingham|Bangor University|London School of Economics and Political Science|University College, London|Lancashire Care NHS Foundation Trust|Newcastle University|King's College London Phase 3 2013-01-01 2015-10-07
    NCT00571064 Mild to Severe Alzheimer's Disease Drug: Donepezil HCl Eisai Inc.|Pfizer Phase 4 2008-01-01 2013-10-29
    NCT01923259 Healthy Drug: Donepezil Dr. Reddy's Laboratories Limited Phase 1 2010-10-01 2013-08-13
    NCT01923558 Healthy Drug: Donepezil Dr. Reddy's Laboratories Limited Phase 1 2010-10-01 2013-08-13
    NCT00220584 Fragile X Syndrome Drug: donepezil Stanford University Phase 1 2005-07-01 2012-12-11
    NCT01042314 Alzheimer Disease Drug: Donepezil|Drug: BMS-708163 Bristol-Myers Squibb Phase 1 2010-01-01 2011-01-24
    NCT02550665 Alzheimer's Disease Drug: donepezil Asan Medical Center|Dong-A University|Myongji Hospital|Seoul National University Bundang Hospital|Seoul St. Mary's Hospital|Chung-Ang University|Eisai Inc. Phase 3 2014-12-01 2016-07-15
    NCT02222727 Aneurysmal Subarachnoid Hemorrhage|Delayed Neurological Deficit|Delayed Cerebral Ischemia|Vasospasm Drug: Donepezil St George's, University of London Phase 2 2014-01-01 2016-05-03
    NCT00352664 Advanced Cancer Drug: Donepezil|Drug: Placebo M.D. Anderson Cancer Center|Pfizer Phase 3 2003-11-01 2016-04-05
    NCT01951118 Alzheimer Disease|Mild Cognitive Impairment|Delirium, Dementia, Amnestic, Cognitive Disorders Drug: Donepezil New York State Psychiatric Institute|National Institutes of Health (NIH)|National Institute on Aging (NIA) Phase 4 2013-10-01 2016-12-27
    NCT01297036 Alzheimer Disease Drug: Donepezil, ODT 10 mg|Drug: Donepezil, 10 mg tablet Korea University Anam Hospital|Chong Kun Dang Pharmaceutical Corp. Phase 1 2008-01-01 2011-02-15
    NCT01278407 Dementia With Lewy Bodies (DLB) Drug: Donepezil 5 mg|Drug: Donepezil 10 mg|Drug: Donepezil matched placebo Eisai Co., Ltd.|Eisai Inc. Phase 3 2011-02-01 2015-12-30
    NCT01276353 Alzheimer's Type Dementia Drug: E2020|Drug: E2020 Eisai Inc. Phase 2 2011-01-01 2014-08-05

    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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