Pharmacological evaluation of [11C]donepezil as a tracer for visualization of acetylcholinesterase by PET |
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| Authors: | De Vos F Santens P Vermeirsch H Dewolf I Dumont F Slegers G Dierckx R A De Reuck J |
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| Affiliation: | Department of Radiopharmacy, University Hospital of Gent, Gent, Belgium. filipx.devos@rug.ac.be |
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| Abstract: | Donepezil is a highly potent and selective reversible achetylcholinesterase inhibitor. [(11)C]Donepezil is prepared by methylation with [(11)C]CH(3)I 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 (11)C-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. |
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