000894996 001__ 894996
000894996 005__ 20210930133543.0
000894996 0247_ $$2doi$$a10.1021/acschemneuro.1c00284
000894996 0247_ $$2Handle$$a2128/28655
000894996 0247_ $$2pmid$$a34449193
000894996 0247_ $$2WOS$$aWOS:000697282400006
000894996 037__ $$aFZJ-2021-03517
000894996 082__ $$a540
000894996 1001_ $$0P:(DE-Juel1)180770$$aHoffmann, Chris$$b0$$ufzj
000894996 245__ $$a[18F]ALX5406: A Brain-Penetrating Prodrug for GlyT1-Specific PET Imaging
000894996 260__ $$aWashington, DC$$bACS Publ.$$c2021
000894996 3367_ $$2DRIVER$$aarticle
000894996 3367_ $$2DataCite$$aOutput Types/Journal article
000894996 3367_ $$0PUB:(DE-HGF)16$$2PUB:(DE-HGF)$$aJournal Article$$bjournal$$mjournal$$s1631791650_6695
000894996 3367_ $$2BibTeX$$aARTICLE
000894996 3367_ $$2ORCID$$aJOURNAL_ARTICLE
000894996 3367_ $$00$$2EndNote$$aJournal Article
000894996 520__ $$aSelective inhibition of glycine transporter 1 (GlyT1) has emerged as a potential approach to alleviate N-methyl-D-aspartate receptor (NMDAR) hypofunction in patients with schizophrenia and cognitive decline. ALX5407 is a potent and selective inhibitor of GlyT1 derived from the metabolic intermediate sarcosine (N-methylglycine) that showed antipsychotic potential in a number of animal models. Whereas clinical application of ALX5407 is limited by adverse effects on motor performance and respiratoryfunction, a suitably radiolabeled drug could represent a promising PET tracer for the visualization of GlyT1 in the brain. Herein, [18F]ALX5407 and the corresponding methyl ester, [18F]ALX5406, were prepared by alcoholenhanced copper mediated radiofluorination and studied in vitro in rat brain slices and in vivo in normal rats. [18F]ALX5407 demonstrated accumulation consistent with the distribution of GlyT1 in in vitro autoradiographic studies but no brain uptake in μPET experiments in naıv̈ e rats. In contrast, the methyl ester [18F]ALX5406 rapidly entered the brain and was enzymatically transformed into [18F]ALX5407, resulting in a regional accumulation pattern consistent with GlyT1 specific binding. We conclude that [18F]ALX5406 is a promising and easily accessible PET probe for preclinical in vivo imaging of GlyT1 in the brain.
000894996 536__ $$0G:(DE-HGF)POF4-5253$$a5253 - Neuroimaging (POF4-525)$$cPOF4-525$$fPOF IV$$x0
000894996 588__ $$aDataset connected to CrossRef, Journals: juser.fz-juelich.de
000894996 7001_ $$0P:(DE-Juel1)165360$$aEvcüman, Sibel$$b1$$ufzj
000894996 7001_ $$0P:(DE-Juel1)175142$$aNeumaier, Felix$$b2$$ufzj
000894996 7001_ $$0P:(DE-Juel1)176188$$aZlatopolskiy, Boris D.$$b3
000894996 7001_ $$0P:(DE-Juel1)132740$$aHumpert, Swen$$b4$$ufzj
000894996 7001_ $$0P:(DE-Juel1)131810$$aBier, Dirk$$b5
000894996 7001_ $$0P:(DE-Juel1)131824$$aHolschbach, Marcus$$b6$$ufzj
000894996 7001_ $$0P:(DE-Juel1)131847$$aSchulze, Annette$$b7$$ufzj
000894996 7001_ $$0P:(DE-Juel1)180330$$aEndepols, Heike$$b8$$ufzj
000894996 7001_ $$0P:(DE-Juel1)166419$$aNeumaier, Bernd$$b9$$eCorresponding author
000894996 773__ $$0PERI:(DE-600)2528493-9$$a10.1021/acschemneuro.1c00284$$gVol. 12, no. 18, p. 3335 - 3346$$n18$$p3335 - 3346$$tACS chemical neuroscience$$v12$$x1948-7193$$y2021
000894996 8564_ $$uhttps://juser.fz-juelich.de/record/894996/files/Autorenversion.pdf$$yPublished on 2021-08-27. Available in OpenAccess from 2022-08-27.
000894996 8564_ $$uhttps://juser.fz-juelich.de/record/894996/files/Supporting%20Information.pdf$$yPublished on 2021-08-27. Available in OpenAccess from 2022-08-27.
000894996 8564_ $$uhttps://juser.fz-juelich.de/record/894996/files/acschemneuro.1c00284.pdf$$yRestricted
000894996 909CO $$ooai:juser.fz-juelich.de:894996$$pdnbdelivery$$pdriver$$pVDB$$popen_access$$popenaire
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)180770$$aForschungszentrum Jülich$$b0$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)165360$$aForschungszentrum Jülich$$b1$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)175142$$aForschungszentrum Jülich$$b2$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)132740$$aForschungszentrum Jülich$$b4$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)131810$$aForschungszentrum Jülich$$b5$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)131824$$aForschungszentrum Jülich$$b6$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)131847$$aForschungszentrum Jülich$$b7$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)180330$$aForschungszentrum Jülich$$b8$$kFZJ
000894996 9101_ $$0I:(DE-588b)5008462-8$$6P:(DE-Juel1)166419$$aForschungszentrum Jülich$$b9$$kFZJ
000894996 9131_ $$0G:(DE-HGF)POF4-525$$1G:(DE-HGF)POF4-520$$2G:(DE-HGF)POF4-500$$3G:(DE-HGF)POF4$$4G:(DE-HGF)POF$$9G:(DE-HGF)POF4-5253$$aDE-HGF$$bKey Technologies$$lNatural, Artificial and Cognitive Information Processing$$vDecoding Brain Organization and Dysfunction$$x0
000894996 9141_ $$y2021
000894996 915__ $$0StatID:(DE-HGF)0200$$2StatID$$aDBCoverage$$bSCOPUS$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)0300$$2StatID$$aDBCoverage$$bMedline$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)1050$$2StatID$$aDBCoverage$$bBIOSIS Previews$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)1190$$2StatID$$aDBCoverage$$bBiological Abstracts$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)0530$$2StatID$$aEmbargoed OpenAccess
000894996 915__ $$0StatID:(DE-HGF)0100$$2StatID$$aJCR$$bACS CHEM NEUROSCI : 2019$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)0113$$2StatID$$aWoS$$bScience Citation Index Expanded$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)0150$$2StatID$$aDBCoverage$$bWeb of Science Core Collection$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)9900$$2StatID$$aIF < 5$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)0160$$2StatID$$aDBCoverage$$bEssential Science Indicators$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)0320$$2StatID$$aDBCoverage$$bPubMed Central$$d2021-02-03
000894996 915__ $$0StatID:(DE-HGF)0199$$2StatID$$aDBCoverage$$bClarivate Analytics Master Journal List$$d2021-02-03
000894996 920__ $$lyes
000894996 9201_ $$0I:(DE-Juel1)INM-5-20090406$$kINM-5$$lNuklearchemie$$x0
000894996 980__ $$ajournal
000894996 980__ $$aVDB
000894996 980__ $$aUNRESTRICTED
000894996 980__ $$aI:(DE-Juel1)INM-5-20090406
000894996 9801_ $$aFullTexts