Effect of donepezil on brain acetylcholinesterase activity in patients with AD measured by PET

• Published in: Neurology Vol. 56; no. 3; pp. 408 - 410
• Main Authors: SHINOTOH, H, AOTSUKA, A, FUKUSHI, K, NAGATSUKA, S, TANAKA, N, OTA, T, TANADA, S, IRIE, T
• Format: Journal Article
• Language: English
• Published: Hagerstown, MD Lippincott Williams & Wilkins 13-02-2001
• Subjects: Acetylcholinesterase - metabolism; Aged; Alzheimer Disease - diagnostic imaging; Alzheimer Disease - enzymology; Biological and medical sciences; Brain - diagnostic imaging; Brain - enzymology; Degenerative and inherited degenerative diseases of the nervous system. Leukodystrophies. Prion diseases; Donepezil; Female; Humans; Indans - therapeutic use; Male; Medical sciences; Middle Aged; Neurology; Piperidines - therapeutic use; Time Factors; Tomography, Emission-Computed; Radionuclide study; Human; Nervous system diseases; Enzyme; Alzheimer disease; Central nervous system; Exploration; Esterases; Acetylcholinesterase; Carboxylic ester hydrolases; Cerebral disorder; Enzymatic activity; Donepezil; Central nervous system disease; Piperidine derivatives; Hydrolases; Degenerative disease; Brain (vertebrata); Positron; Emission tomography
• ISSN: 0028-3878; 1526-632X
• DOI: 10.1212/WNL.56.3.408

Acetylcholinesterase (AChE) activities in the brain of three patients with AD were measured once before and once during donepezil treatment (5 mg/d in two patients, 3 mg/d in one patient) using PET and N-[11C]methylpiperidin-4-yl acetate. Donepezil reduced k(3) values, an index of AChE activity, in the cerebral cortex by 39 +/- 5%. All patients showed some degree of symptomatic improvement, and it was concluded that this improvement was likely caused by improved cholinergic activity by inhibition of AChE in the brain.