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。
Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
18 μM/kg 腹腔注射或口服给药
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。
[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
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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