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Radiopharmaceutical Chemistry: New Chemistry-NeurosciencesNew Chemistry-Neurosciences Posters |
1 Laboratory of Radiopharmacy, University Ghent, Gent, Oost Vlaanderen, Belgium; 2 Chemical Biology Research Branch, National Institute on Drug Abuse and National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland
1216
Objectives: The aim of this study was to evaluate the usefulness of [123I]-(4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(4-iodobenzyl)piperidine ([123I]-(1)) as an in vivo tracer for the dopamine transporter.
Methods: [123I]-(1) was synthesized by electrophilic substitution. A biodistribution was performed in male NMRI mice (n=3). Mice were injected i.v. with approximately 5 µCi (185 kBq) [123I]-(1). At various time points p.i., the mice were sacrificed and dissected. At 10 min (n=2) and 1 h (n=4) p.i., a metabolite analysis was performed. Mice were injected with 50-100 µCi (1.85-3.7 MBq) [123I]-(1). Blood, brain and urine were removed and extracted with acetonitrile. Supernatant was drawn off and analyzed by RP HPLC.
Results: Biodistribution studies showed brain uptake of 0.96 % ID/g at 30 sec p.i. and 0.26 % ID/g at 3 h p.i. High blood activity was observed at all time points. Extraction efficiencies of plasma, brain and urine were 80 %, 79 % and 92 %, respectively. The fraction of radioactivity in plasma that represents [123I]-(1) was 63 % at 10 min p.i. and 55.5 % at 1 h p.i. At 10 min p.i., 85 % of parent compound remained in the brain and at 1 h p.i. 83% was still present. The radioactivity in the urine was > 95 % due to free iodine.
Conclusions: These results indicate that [123I]-(1) passes the BBB, displaying a good metabolic profile. Further evaluation of [123I]-(1) as a potential SPECT tracer for DAT is necessary.
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