Pharmacological evaluation of [11C]donepezil as a tracer for visualization of acetylcholinesterase by PET.
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.
De Vos
F
F
Department of Radiopharmacy, University Hospital of Gent, Gent, Belgium. filipx.devos@rug.ac.be
Santens
P
P
Vermeirsch
H
H
Dewolf
I
I
Dumont
F
F
Slegers
G
G
Dierckx
R A
RA
De Reuck J
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000000981:diagnostic imaging / Q000201:enzymology / Q000378:metabolism; D002250:Carbon Radioisotopes; D002800:Cholinesterase Inhibitors / Q000493:pharmacokinetics; D000077265:Donepezil; D005260:Female; D007189:Indans / Q000493:pharmacokinetics; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D010880:Piperidines / Q000493:pharmacokinetics; D011817:Rabbits; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D002800:Cholinesterase Inhibitors; D007189:Indans; D010880:Piperidines; D019275:Radiopharmaceuticals; D000077265:Donepezil; D000110:Acetylcholinesterase