First Evaluation in Humans of [123I]PE2I: A Selective Radioligand for Visualization of the Striatal Dopamine Transporter Density
(E)-N-(3-iodoprop-2-enyl)-2β-Carbomethoxy-3β-(4-methylphenyl)nortropane (PE2I) is recently synthesised selective compound for the dopamine transporter. In the present study 123I-labelled PE2I were prepared for SPET studies with healthy volunteers. There was a rapid uptake of radioactivity in brain (3% of ID at 1 hour) and a high accumulation of radioactivity in the striatum. In the thalamus and in cortical regions no visible uptake of radioactivity was observed. Striatum-to-cerebellum ratio was 5 at 70 min. Percentage of unchanged [123I]PE2I in plasma was less than 20% at 1 h post injection. In conclusion, [123I]PE2I is a potential radioligand for the dopamine transporter imaging with SPET.
KeywordsPositron Emission Tomography Dopamine Transporter Gradient HPLC Selective Compound SPET Study
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- 5.Emond P, Garreau L, Chalon S, et al. Synthesis and ligand binding of nortropane derivatives: N-substituted-2β-carbomethoxy-3β-(4-iodophenyl)nortropane and N-(3-iodoprop-2E-enyl)-2β-carbomethoxy-3β-(3’,4’-disubstituted-phenyl)nortropane. New high affinity and selective compounds for the dopamine transporter. J Med Chem 1997; 40:1366–1372.PubMedCrossRefGoogle Scholar
- 6.Guilloteau D, Emond P, Baulieu J-L, et al. Exploration of the dopamine transporter: Invitro and in vivo characterization of a high affinity and high specificity iodinated tropane derivative (E)-N-(3-iodoprop-2-enyl)-2βcarbomethoxy-3β(4’methylphenyl)nortropane or PE2I. Nucl Med Biol (in press).Google Scholar
- 8.Halldin C, Lundkvist C, Guilloteau D, et al. The first selective dopamine transporter radioligand suitable for quantitation with both PET and SPET. Eur J Nucl Med 1997; 24:1057.Google Scholar
- 9.Hall H, Halldin C, Guilloteau D, et al. Dopamine transporters in the post-mortem human brain. Autoradiographic localisation using [125I]PE2I. Eur J Nucl Med 1997; 24:880.Google Scholar