1-Benzyl-4-methylpiperidinyl moiety in donepezil: The priority ticket across the blood-brain-barrier in rats
Abstract
Donepezil (Aricept(R), Pfizer) is an acetylcholinesterase (AChE, E.C. 3.1.1.7) inhibitor (AChEI) widely used in the treatment of Alzheimer's disease (AD). The AChE inhibition increases the level of acetylcholine (ACh) in the synaptic cleft causing higher stimulation of cholinergic receptors in the brain.
The key role of donepezil in AD therapy is stabilization of cognitive functions. The other beneficial effects were discovered during clinical trials: improvement of daily-living activities and neuropsychiatric symptoms such as hallucinations, distractibility, aberrant motor behaviour and apathy.
Based on this knowledge, donepezil may also be applied in vascular dementia, Parkinson's disease and dementia with Lewy bodies and cognitive symptoms associated with multiple sclerosis.