Pharmacological evaluation of [¹¹c]donepezil as tracer for visualization of acetylcholinesterase by PET

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• 作者：De Vos ; F. ; Santens ; P. ; Vermeirsch ; H. ; Dewolf ; I. ; Dumont ; F. ; Slegers ; G. ; Dierckx ; R.A. ; De Reuck ; J.
• 关键词：[¹¹C]donepezil ; Acetylcholinesterase ; PET ; Alzheimer’ ; s
• 刊名：Nuclear Medicine and Biology
• 出版年：2000
• 期刊代码：43_09698051
• 类别：ph
• 出版时间：November, 2000
• 卷：27
• 期：8
• 页码：745-747
• 文件大小：227 K

摘要

Donepezil is a highly potent and selective reversible achetylcholinesterase inhibitor. [¹¹C]Donepezil is prepared by methylation with [¹¹C]CH₃I of the corresponding 6′-O-desmethylprecursor. Tissue distribution in mice revealed a high uptake in brain and rapid clearance from the blood. Metabolization studies in mice indicated the formation of one ¹¹C-labeled polar metabolite that didn’t penetrate the blood-brain barrier. Regional brain distribution in rabbits didn’t reflect the measured achetylcholinesterase distribution in rabbit brain.