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.1 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.
1
Muñoz-Torrero, D. Acetylcholinesterase inhibitors as disease-modifying therapies for Alzheimer’s disease. Curr Med Chem152433-2455(2008).
Mancini, F., Naldi, M., Cavrini, V., et al. Multiwell fluorometric and colorimetric microassays for the evaluation of beta-secretase (BACE-1) inhibitors. Anal Bioanal Chem3881175-1183(2007).
Muñoz-Torrero, D. Acetylcholinesterase inhibitors as disease-modifying therapies for Alzheimer’s disease. Curr Med Chem152433-2455(2008).
Rodríguez-Franco, M.I., Fernández-Bachiller, M.I., Pérez, C., et al. Design and synthesis of N-benzylpiperidine-purine derivatives as new dual inhibitors of acetyl- and butyrylcholinesterase. Bioorg Med Chem136795-6802(2005).
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