"目录号: HY-14566
Donepezil(E 2020)是AChE抑制剂，对bAChE和hAChE的IC50分别为8.12 nM和11.6 nM。
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Galanthamine-Donepezil Hydrochloride-Rivastigmine-(-)-Huperzine A-(±)-Huperzine A-Aldicarb-Edrophonium chloride-sn-Glycero-3-phosphocholine-Benzethonium chloride-4-Methylbenzylidene camphor-Epiberberine chloride-Galanthaminone-Itopride hydrochloride-Pyridostigmine D6 bromide-Imperatorin-
生物活性
Description
Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.Target: AChEDonepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively [1]. Donepezil inhibits the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells in a concentration dependent manner, indicating that Donepezil have muscarinic antagonist activity. Intraperitoneal administration of Donepezil in rats produces a dose dependent increase in salivation and tremor, which are overt cholinergic behavioural signs, with an ED50 of 6 μmol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 μmol/kg following oral administration [2]. A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular and cerebrovascular diseases [3].
Clinical Trial
BeerYaakov Mental Health Center
Schizophrenia-Schizoaffective Disorder-Schizophreniform Disorder
May 2007
Phase 4
Merck Sharp & Dohme Corp.
Alzheimer's Disease
April 2014
Phase 2
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
Parkinson's Disease
January 2013
Phase 3
Beijing Friendship Hospital
Alzheimer's Disease
May 2016
Phase 4
Stanford University
Fragile X Syndrome
July 2005
Phase 1
Teva Pharmaceuticals USA
Healthy
June 2007
Phase 1
Teva Pharmaceuticals USA
Healthy
June 2007
Phase 1
Eisai Inc.-Pfizer
Alzheimer's Disease
July 2007
Phase 4
Kessler Foundation-Pfizer
Stroke-Vascular Dementia-Memory Deficits
May 2007
Phase 1
Asan Medical Center-Dong-A University-Myongji Hospital-Seoul National University Bundang Hospital-Seoul St. Mary's Hospital-Chung-Ang University-Eisai Inc.
Alzheimer's Disease
December 2014
Phase 3
Dr. Reddy's Laboratories Limited
Healthy
October 2010
Phase 1
Dr. Reddy's Laboratories Limited
Healthy
October 2010
Phase 1
St George's, University of London
Aneurysmal Subarachnoid Hemorrhage-Delayed Neurological Deficit-Delayed Cerebral Ischemia-Vasospasm
January 2014
Phase 2
New York State Psychiatric Institute-National Institutes of Health (NIH)-National Institute on Aging (NIA)
Alzheimer Disease-Mild Cognitive Impairment-Delirium, Dementia, Amnestic, Cognitive Disorders
October 2013
Phase 4
Korea University Anam Hospital-Chong Kun Dang Pharmaceutical Corp.
Alzheimer Disease
January 2008
Phase 1
M.D. Anderson Cancer Center-Pfizer
Advanced Cancer
November 2003
Phase 3
Baylor College of Medicine-Spaulding Rehabilitation Hospital-Albert Einstein Healthcare Network-Indiana University-Craig Hospital-TIRR Memorial Hermann
Traumatic Brain Injury-Memory Deficits
September 2014
Phase 3
Per Borghammer-Lundbeck Foundation-University of Aarhus
Parkinson's Disease
May 2013
Phase 1
University of Sao Paulo
Elderly-Delirium of Unknown (Axis III) Etiology-Intensive Care (ICU) Myopathy
August 2012
Phase 4
Wake Forest University Health Sciences-National Cancer Institute (NCI)
Brain Tumors-Metastatic Disease
January 2008
Phase 3
Teva Pharmaceuticals USA
Healthy
April 2006
Phase 1
Teva Pharmaceuticals USA
Healthy
April 2006
Phase 1
Oregon Health and Science University
Parkinson's Disease
December 2011
Phase 4
Memorial Sloan Kettering Cancer Center-Weill Medical College of Cornell University
Brain Tumor-Brain Cancer-Cns Cancer-Cognitive Dysfunction
October 2004
Phase 1
Associacao Fundo de Incentivo a Psicofarmcologia-Fundação de Amparo à Pesquisa do Estado de São Paulo
Obstructive Sleep Apnea
March 2007
Phase 4
Bristol-Myers Squibb
Alzheimer Disease
January 2010
Phase 1
Vanderbilt University
Alzheimer's Disease
December 2006
Phase 1-Phase 2
Shanghai Mental Health Center-The Davis Foundations
Bipolar Disorder-Mania
May 2005
Phase 4
VA Office of Research and Development
Cocaine Abuse and Dependence
February 2007
Phase 2
Eisai Co., Ltd.-Eisai Inc.
Dementia Associated With Cerebrovascular Disease
August 5, 2013
Phase 4
Eisai Inc.-Pfizer
Down Syndrome-Cognitive Dysfunction
September 2008
Phase 3
Dr. Reddy's Laboratories Limited
Healthy
October 2009
Phase 1
Dr. Reddy's Laboratories Limited
Healthy
October 2009
Phase 1
Samsung Medical Center-Eisai Korea Inc.
Alzheimer's Disease-Dementia
March 2007
National Eye Institute (NEI)
Amblyopia
May 1, 2012
Phase 4
Imperial College London-International Stem Cell Forum
Acute Stroke
November 2011
Phase 1-Phase 2
Wake Forest University-National Institute of Neurological Disorders and Stroke (NINDS)-Wake Forest University Health Sciences
Neuropathic Pain
December 2012
Phase 4
Central South University
Impaired Cognition-Schizophrenia
June 2011
Phase 4
Pfizer
Alzheimer's Disease
February 2007
Phase 4
Inje University
Parkinson's Disease
July 2015
Phase 2
Porter Adventist Hospital
Memory Impairment
June 2015
Lawson Health Research Institute
Falls-Gait-Balance-Mild Cognitive Impairment (MCI)
September 2009
Eisai Inc.
Migraine Headache
January 2003
Phase 2
Guang'anmen Hospital of China Academy of Chinese Medical Sciences
Cognitive Impairment
June 2017
Phase 2
Samsung Medical Center-Eisai Korea Inc.
Alzheimer's Disease-Dementia
February 2008
Eisai Korea Inc.-Eisai Inc.
Alzheimer's Disease
February 2014
Phase 4
Eisai Co., Ltd.-Eisai Inc.
End-Stage Renal Disease
February 2010
Phase 4
Eisai Inc.-Eisai Limited
Alzheimer's Disease
June 2007
