000865229 001__ 865229
000865229 005__ 20210130002950.0
000865229 0247_ $$2Handle$$a2128/23007
000865229 037__ $$aFZJ-2019-04760
000865229 041__ $$aEnglish
000865229 1001_ $$0P:(DE-Juel1)173964$$aWillmann, Michael$$b0$$eCorresponding author$$ufzj
000865229 1112_ $$aDPhG Annual Meeting 2019$$cHeidelberg$$d2019-09-01 - 2019-09-03$$wGermany
000865229 245__ $$aNovel 18F-labeled D4-receptor ligands
000865229 260__ $$c2019
000865229 3367_ $$033$$2EndNote$$aConference Paper
000865229 3367_ $$2BibTeX$$aINPROCEEDINGS
000865229 3367_ $$2DRIVER$$aconferenceObject
000865229 3367_ $$2ORCID$$aCONFERENCE_POSTER
000865229 3367_ $$2DataCite$$aOutput Types/Conference Poster
000865229 3367_ $$0PUB:(DE-HGF)24$$2PUB:(DE-HGF)$$aPoster$$bposter$$mposter$$s1569412294_25780$$xAfter Call
000865229 520__ $$aThe role of the dopamine D4-receptor subtype in the development of neurodegenerative diseases such as schizophrenia has been discussed for several decades. Specific radiotracers for more detailed preclinical and clinical investigations are still missing so far. The objective of this study was to develop D4-selective radioligands for positron emission tomography (PET). The selected lead structures exhibit high D4R subtype selectivity and a suitable LogP values, rendering them attractive for the development of a D4-selective radioligand for PET-imaging. Two D4R-ligands, know from literature, were selected for labeling with fluorine-18 (t1/2=108 min), the most ideal positron emitting nuclide.D4R-radioligand [18F]I was synthesized from 2-[18F]fluorophenylpiperazine 2, obtained by an alcohol enhanced Cu(II)-mediated radiofluorination of the Boc-protected precursor 1 followed by deprotection of the radiolabeled intermediate with TFA. Subsequently, [18F]I was obtained by reductive amination with 3 in a total isolated radiochemical yield of 7 % within 2 h. Three independent auto radiographic studies with molar activities up to 90 GBq/µmol showed high content of non-specific binding that covers any possible specific binding. The chiral D4R-radioligand [18F]II was also obtained by alcohol enhanced Cu(II)-mediated radiofluorination of the boronic acid precursor 4 in a RCY of 66±5 % within 60 min after isolation by semi-preparative HPLC. Preliminary in vitro autoradiographic study indicates specific binding of [18F]II in areas with D4-expression, consistent with results published earlier.
000865229 536__ $$0G:(DE-HGF)POF3-573$$a573 - Neuroimaging (POF3-573)$$cPOF3-573$$fPOF III$$x0
000865229 7001_ $$0P:(DE-Juel1)131818$$aErmert, Johannes$$b1$$ufzj
000865229 7001_ $$0P:(DE-Juel1)166419$$aNeumaier, Bernd$$b2$$ufzj
000865229 8564_ $$uhttps://juser.fz-juelich.de/record/865229/files/Abstract%20DPhG%202019%20Heidelberg_Willmann.pdf$$yOpenAccess
000865229 8564_ $$uhttps://juser.fz-juelich.de/record/865229/files/Poster.pdf$$yOpenAccess
000865229 8564_ $$uhttps://juser.fz-juelich.de/record/865229/files/Abstract%20DPhG%202019%20Heidelberg_Willmann.pdf?subformat=pdfa$$xpdfa$$yOpenAccess
000865229 8564_ $$uhttps://juser.fz-juelich.de/record/865229/files/Poster.pdf?subformat=pdfa$$xpdfa$$yOpenAccess
000865229 909CO $$ooai:juser.fz-juelich.de:865229$$pdriver$$pVDB$$popen_access$$popenaire
000865229 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)173964$$aForschungszentrum Jülich$$b0$$kFZJ
000865229 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)131818$$aForschungszentrum Jülich$$b1$$kFZJ
000865229 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)166419$$aForschungszentrum Jülich$$b2$$kFZJ
000865229 9131_ $$0G:(DE-HGF)POF3-573$$1G:(DE-HGF)POF3-570$$2G:(DE-HGF)POF3-500$$3G:(DE-HGF)POF3$$4G:(DE-HGF)POF$$aDE-HGF$$bKey Technologies$$lDecoding the Human Brain$$vNeuroimaging$$x0
000865229 9141_ $$y2019
000865229 915__ $$0StatID:(DE-HGF)0510$$2StatID$$aOpenAccess
000865229 920__ $$lyes
000865229 9201_ $$0I:(DE-Juel1)INM-5-20090406$$kINM-5$$lNuklearchemie$$x0
000865229 980__ $$aposter
000865229 980__ $$aVDB
000865229 980__ $$aUNRESTRICTED
000865229 980__ $$aI:(DE-Juel1)INM-5-20090406
000865229 9801_ $$aFullTexts