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dc.contributor.authorKimura, Hiroyukien
dc.contributor.authorMatsuda, Hirokazuen
dc.contributor.authorFujimoto, Hiroyukien
dc.contributor.authorArimitsu, Kenjien
dc.contributor.authorToyoda, Kentaroen
dc.contributor.authorMukai, Erien
dc.contributor.authorNakamura, Hiroshien
dc.contributor.authorOgawa, Yuen
dc.contributor.authorTakagi, Mikakoen
dc.contributor.authorOno, Masahiroen
dc.contributor.authorInagaki, Nobuyaen
dc.contributor.authorSaji, Hideoen
dc.contributor.alternative佐治, 英郎ja
dc.date.accessioned2014-07-08T04:10:56Z-
dc.date.available2014-07-08T04:10:56Z-
dc.date.issued2014-07-01-
dc.identifier.issn0968-0896-
dc.identifier.urihttp://hdl.handle.net/2433/188927-
dc.description.abstractMeasuring changes in β-cell mass in vivo during progression of diabetes mellitus is important for understanding the pathogenesis, facilitating early diagnosis, and developing novel therapeutics for this disease. However, a non-invasive method has not been developed. A novel series of mitiglinide derivatives (o-FMIT, m-FMIT and p-FMIT; FMITs) were synthesized and their binding affinity for the sulfonylurea receptor 1 (SUR1) of pancreatic islets were evaluated by inhibition studies. (+)-(S)-o-FMIT had the highest affinity of our synthesized FMITs (IC50=1.8μM). (+)-(S)-o-[(18)F]FMIT was obtained with radiochemical yield of 18% by radiofluorination of racemic precursor 7, hydrolysis, and optical resolution with chiral HPLC; its radiochemical purity was >99%. In biodistribution experiments using normal mice, (+)-(S)-o-[(18)F]FMIT showed 1.94±0.42% ID/g of pancreatic uptake at 5min p.i., and decreases in radioactivity in the liver (located close to the pancreas) was relatively rapid. Ex vivo autoradiography experiments using pancreatic sections confirmed accumulation of (+)-(S)-o-[(18)F]FMIT in pancreatic β-cells. These results suggest that (+)-(S)-o-[(18)F]FMIT meets the basic requirements for an radiotracer, and could be a candidate positron emission tomography tracer for in vivo imaging of pancreatic β-cells.en
dc.format.mimetypeapplication/pdf-
dc.language.isoeng-
dc.publisherElsevier BVen
dc.rights© 2014 Elsevier Ltd.en
dc.rightsThis is not the published version. Please cite only the published version.en
dc.rightsこの論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。ja
dc.subjectMitiglinideen
dc.subjectPositron emission tomography tracersen
dc.subject(18)Fen
dc.subjectSulfonylurea receptor 1en
dc.titleSynthesis and evaluation of 18F-labeled mitiglinide derivatives as positron emission tomography tracers for β-cell imaging.en
dc.typejournal article-
dc.type.niitypeJournal Article-
dc.identifier.ncidAA10938083-
dc.identifier.jtitleBioorganic & medicinal chemistryen
dc.identifier.volume22-
dc.identifier.issue13-
dc.identifier.spage3270-
dc.identifier.epage3278-
dc.relation.doi10.1016/j.bmc.2014.04.059-
dc.textversionauthor-
dc.identifier.pmid24842616-
dcterms.accessRightsopen access-
dc.identifier.pissn0968-0896-
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