Pharmacological evaluation of [C-11]conepezil as tracer for visualization of acetylcholinesterase by PET

Authors
De Vos, F Santens, P Vermeirsch, H Dewolf, I Dumont, F Slegers, G Dierckx, RA De Reuck, J
Citation
F. De Vos et al., Pharmacological evaluation of [C-11]conepezil as tracer for visualization of acetylcholinesterase by PET, NUCL MED BI, 27(8), 2000, pp. 745-747
Citations number
14
Categorie Soggetti
Medical Research Diagnosis & Treatment
Journal title
NUCLEAR MEDICINE AND BIOLOGY
ISSN journal
09698051 → ACNP
Volume
27
Issue
8
Year of publication
2000
Pages
745 - 747
Database
ISI
SICI code
0969-8051(200011)27:8<745:PEO[AT>2.0.ZU;2-M
Abstract
Donepezil is a highly potent and selective reversible achetylcholinesterase inhibitor. [C-11]Donepezil is prepared by methylation with [C-11]CH3I of t he corresponding 6'-O-desmethylprecursor. Tissue distribution in mice revea led a high uptake in brain and rapid clearance from the blood. Metabolizati on studies in mice indicated the formation of one C-11-labeled polar metabo lite that didn't penetrate the blood brain barrier. Regional brain distribu tion in rabbits didn't reflect the measured achetylcholinesterase distribut ion in rabbit brain. NUCL MED BIOL 27;8:745-747, 2000. (C) 2000 Elsevier Sc ience Inc, All rights reserved.