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000889311 1001_ $$0P:(DE-Juel1)173964$$aWillmann, Michael$$b0$$ufzj
000889311 245__ $$aRadiosynthesis and evaluation of 18F-labeled dopamine D4-receptor ligands
000889311 260__ $$aAmsterdam [u.a.]$$bElsevier Science$$c2021
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000889311 520__ $$aIntroductionThe dopamine D4 receptor (D4R) has attracted considerable attention as potential target for the treatment of a broad range of central nervous system disorders. Although many efforts have been made to improve the performance of putative radioligand candidates, there is still a lack of D4R selective tracers suitable for in vivo PET imaging. Thus, the objective of this work was to develop a D4-selective PET ligand for clinical applications.MethodsFour compounds based on previous and new lead structures were prepared and characterized with regard to their D4R subtype selectivity and predicted lipophilicity. From these, 3-((4-(2-fluorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridine I and (S)-4-(3-fluoro-4-methoxybenzyl)-2-(phenoxymethyl)morpholine II were selected for labeling with fluorine-18 and subsequent evaluation by in vitro autoradiography to assess their suitability as D4 radioligand candidates for in vivo imaging.ResultsThe radiosynthesis of [18F]I and [18F]II was successfully achieved by copper-mediated radiofluorination with radiochemical yields of 7% and 66%, respectively. The radioligand [18F]II showed specific binding in areas where D4 expression is expected, whereas [18F]I did not show any uptake in distinct brain regions and exhibited an unacceptable degree of non-specific binding.
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000889311 7001_ $$0P:(DE-Juel1)131818$$aErmert, Johannes$$b1$$eCorresponding author$$ufzj
000889311 7001_ $$0P:(DE-HGF)0$$aPrante, Olaf$$b2
000889311 7001_ $$0P:(DE-HGF)0$$aHübner, Harald$$b3
000889311 7001_ $$0P:(DE-HGF)0$$aGmeiner, Peter$$b4
000889311 7001_ $$0P:(DE-Juel1)166419$$aNeumaier, Bernd$$b5$$ufzj
000889311 773__ $$0PERI:(DE-600)1498538-x$$a10.1016/j.nucmedbio.2020.07.004$$gp. S0969805120301955$$p43-52$$tNuclear medicine and biology$$v92$$x0969-8051$$y2021
000889311 8564_ $$uhttps://juser.fz-juelich.de/record/889311/files/1-s2.0-S0969805120301955-main-2.pdf
000889311 8564_ $$uhttps://juser.fz-juelich.de/record/889311/files/19881CV7-1.pdf
000889311 8564_ $$uhttps://juser.fz-juelich.de/record/889311/files/Autorenmanuskript.pdf$$yPublished on 2020-07-16. Available in OpenAccess from 2021-07-16.
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