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Evaluation of the superselective radioligand [123I]PE2I for imaging of the dopamine transporter in SPECT: PhD Thesis

Research output: Book/ReportPh.D. thesisResearch

  1. Epilepsikirurgi

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Design of Infusion Schemes for Neuroreceptor Imaging: Application to [(11)C]Flumazenil-PET Steady-State Study

    Research output: Contribution to journalJournal articleResearchpeer-review

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Imaging of the dopamine transporter (DAT) with Single Photon Emission Computer Tomography (SPECT) has increasingly been used as a biomarker for the integrity of presynaptic dopaminergic nerve cells in patients with movement disorders. 123-I-labelled N-(3-iodoprop-2E-enyl)-2-β-carbomethoxy-3β-(4-methylphenyl) nortropane, named PE2I, is a relatively new radioligand that has about 10-fold higher in vitro selectivity for the DAT than for the serotonin transporter (SERT) compared to the slightly older but very used and licensed radioligand [123I]FP-CIT (DaTSCAN). Further [123I]PE2I has faster kinetics than [123I]FP-CIT. Because of its fast kinetic properties, quantification of [123I]PE2I binding to DAT is possible using kinetic or graphical analysis following bolus injection of tracer or as a combination of bolus and constant infusion. Based on preliminary bolus trials we have been able to calculate a B/I ratio of [123I]PE2I. This B/I ratio (2.7h) gave rise to steady state conditions and excellent reproducibility. Further, manual delineation of ROI directly on SPECT images performed equally well to a MRI-defined probability map based ROI delineation in terms of intrasubject variability of binding potential of DAT. Finally the in vivo SERT binding in DAT images obtained with [123I]FP-CIT was significant as compared to the [123I]PE2I image. [123I]PE2I is a super selective SPECT DAT radioligand with optimal kinetic properties for accurate quantification of the DAT availability in striatum. Apart from the more laborious B/I design it is currently to be considered the best radioligand for imaging the DAT in the human brain with SPECT.
Original languageEnglish
Place of PublicationKøbenhavn
PublisherEget Forlag
Number of pages106
Publication statusPublished - 18 Mar 2011

ID: 33249127