|Place of Origin:||CHINA|
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pharmaceutical active ingredients,
pharmaceutical fine chemicals
Product Name: Donepezil
Synonyms: 2-[(1-benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL) METHYL] PIPERIDINE;AKOS 226-23;2,3-dihydro-5,6-dimethoxy-2-((1-(phenylmethyl)-4-piperidinyl)methyl)-1h-inde;n-1-one;N-Benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl] piperidine;5,6-Dimethoxy-2,3-dihydro-1H-inden-1-one
Melting point: 207°C
Water Solubility: 2.931 mg/L
Donepezil is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.
Acetylcholine is a neurotransmitter involved in neural signaling throughout the body. Donepezil is a reversible acetylcholinesterase inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine. It has a half-life in circulation of about 70 hours. As acetylcholine modulates plasticity, excitability, and arousal in the central nervous system, donepezil is commonly used in the treatment of Alzheimer’s disease to improve cognition, memory, and behavior. In this way, it is intended to prevent or reverse dementia. Studies on these effects have been equivocal, indicating that more research into the therapeutic potential of donepezil is warranted.
Donepezil is a centrally acting reversible acetylcholinesterase inhibitor. Its main
therapeutic use is in the palliative treatment of Alzheimer's disease. Common side effects
include gastrointestinal upset. It has an oral bioavailability of 100% and easily crosses
the blood-brain barrier. Because it has a biological half-life of about 70 hours, it can be
taken once a day.
Donepezil has been tested in other cognitive disorders (and is sometimes used off label)
including Lewy body dementia and vascular dementia, but it is not currently approved for
these indications. Donepezil has been found to improve sleep apnea in Alzheimer's patients.
Donepezil has also been studied in patients with Mild Cognitive Impairment, schizophrenia,
attention deficit disorder, post-coronary bypass cognitive impairment, cognitive impairment
associated with multiple sclerosis, CADASIL, and Down syndrome.
A 3 year NIH trial in patients with mild cognitive impairment reported that donepezil was
superior to placebo in delaying rate of progression to dementia during the initial 18
months of the study but this was not sustained at 36 months. In a secondary analysis, a
subgroup of individuals with the Apolipoprotein E4 genotype showed sustained benefits with
donepezil throughout the study. However at this time donepezil is not indicated for
prevention of dementia. Recent studies suggest that Donepezil can improve speech in
children with autism. The studies found that speech of autistic children who were mild to
moderately affected appeared to improve from the use of Donepezil.