Synthesis and biological characterization of stable and radioiodinated (±)-trans-2-hydroxy-3P{4-(3-iodophenyl)piperidyl}-1,2,3,4-tetrahydronaphthalene (3-IBVM)

Donepezil is a highly potent and selective reversible achetylcholinesterase inhibitor. [11C] Donepezil is prepared by methylation with [11C]CH3I of the corresponding 6ʹ-Odesmethylprecursor. 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 11Clabeled polar metabolite that didnʹt penetrate the blood-brain barrier. Regional brain distribution in rabbits didnʹt reflect the measured achetylcholinesterase distribution in rabbit brain.