Book/Dissertation / PhD Thesis

FZJ-2021-04358

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Synthese 18F-markierter PET-Tracer durch nukleophile Kupfer-vermittelte Radiofluorierung

Evcüman, S. (Corresponding author)FZJ*

2021
Forschungszentrum Jülich GmbH Zentralbibliothek, Verlag Jülich

Please use a persistent id in citations: http://hdl.handle.net/2128/30107

Report No.: 4430

Abstract: Positron emission tomography (PET) enables to detect physiological and pathophysiological processeson the cellular or molecular level. Therefore, PET has gained great importance as a diagnostic imagingtechnique. Thus, a number of neurological and neoplastic disordes are associated with alterations inthe expression or activity of certain receptors, transporters or enzymes, which can be visualized andquantified using PET imaging. This is achieved by the application of radiolabeled probes (tracers) thatselectively interact with a molecular target of interest and can be detected non-invasively based onthe emission of positrons. Owing to its favorable half-live and the low energy of emitted positrons,fluorine-18 is one of the most attractive radionuclides for labeling of PET-tracers. A number of noveltransition metal-mediated, late-stage radiofluorination methods have enabled an easy access to 18Flabeledaromatic systems regardless of their electronic properties. In particular, Cu-mediatedradiofluorination with alcohols as co-solvents has been shown to afford high radiochemical yields(RCYs) of several clinically relevant PET tracers that are hardly or not accessible by conventionalmethods.The aim of the present work was to prepare 18F-labeled PET tracers for different molecular targets byalcohol-enhanced Cu-mediated radiofluorination and to evaluate their properties by preclinicalexperiments in vitro and in vivo. The molecular targets were selected based on their pathophysiologicalrelevance and comprised the glycine transporter 1 (GlyT1), the synaptic vesicle glycoprotein 2A (SV2A)and the A1 adenosine receptor (A1AR). Following identification of suitable high-affinity lead structures,the corresponding precursor compounds were synthesized and subsequently radiolabeled usingcopper-mediated radiofluorination.

Note: Dissertation, Univ. Köln, 2021

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Contributing Institute(s):

1. Nuklearchemie (INM-5)

Research Program(s):

1. 5253 - Neuroimaging (POF4-525) (POF4-525)

Appears in the scientific report 2021

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Database coverage:
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