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| 005 | 20220930130303.0 | ||
| 024 | 7 | _ | |a 10.1016/j.nucmedbio.2020.07.004 |2 doi |
| 024 | 7 | _ | |a 0969-8051 |2 ISSN |
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| 037 | _ | _ | |a FZJ-2021-00203 |
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| 100 | 1 | _ | |a Willmann, Michael |0 P:(DE-Juel1)173964 |b 0 |u fzj |
| 245 | _ | _ | |a Radiosynthesis and evaluation of 18F-labeled dopamine D4-receptor ligands |
| 260 | _ | _ | |a Amsterdam [u.a.] |c 2021 |b Elsevier Science |
| 336 | 7 | _ | |a article |2 DRIVER |
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| 520 | _ | _ | |a IntroductionThe 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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| 700 | 1 | _ | |a Ermert, Johannes |0 P:(DE-Juel1)131818 |b 1 |e Corresponding author |u fzj |
| 700 | 1 | _ | |a Prante, Olaf |0 P:(DE-HGF)0 |b 2 |
| 700 | 1 | _ | |a Hübner, Harald |0 P:(DE-HGF)0 |b 3 |
| 700 | 1 | _ | |a Gmeiner, Peter |0 P:(DE-HGF)0 |b 4 |
| 700 | 1 | _ | |a Neumaier, Bernd |0 P:(DE-Juel1)166419 |b 5 |u fzj |
| 773 | _ | _ | |a 10.1016/j.nucmedbio.2020.07.004 |g p. S0969805120301955 |0 PERI:(DE-600)1498538-x |p 43-52 |t Nuclear medicine and biology |v 92 |y 2021 |x 0969-8051 |
| 856 | 4 | _ | |u https://juser.fz-juelich.de/record/889311/files/1-s2.0-S0969805120301955-main-2.pdf |
| 856 | 4 | _ | |u https://juser.fz-juelich.de/record/889311/files/19881CV7-1.pdf |
| 856 | 4 | _ | |y Published on 2020-07-16. Available in OpenAccess from 2021-07-16. |u https://juser.fz-juelich.de/record/889311/files/Autorenmanuskript.pdf |
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