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dc.contributor.author | Kimura, Hiroyuki | en |
dc.contributor.author | Matsuda, Hirokazu | en |
dc.contributor.author | Fujimoto, Hiroyuki | en |
dc.contributor.author | Arimitsu, Kenji | en |
dc.contributor.author | Toyoda, Kentaro | en |
dc.contributor.author | Mukai, Eri | en |
dc.contributor.author | Nakamura, Hiroshi | en |
dc.contributor.author | Ogawa, Yu | en |
dc.contributor.author | Takagi, Mikako | en |
dc.contributor.author | Ono, Masahiro | en |
dc.contributor.author | Inagaki, Nobuya | en |
dc.contributor.author | Saji, Hideo | en |
dc.contributor.alternative | 佐治, 英郎 | ja |
dc.date.accessioned | 2014-07-08T04:10:56Z | - |
dc.date.available | 2014-07-08T04:10:56Z | - |
dc.date.issued | 2014-07-01 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://hdl.handle.net/2433/188927 | - |
dc.description.abstract | Measuring 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.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier BV | en |
dc.rights | © 2014 Elsevier Ltd. | en |
dc.rights | This 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.subject | Mitiglinide | en |
dc.subject | Positron emission tomography tracers | en |
dc.subject | (18)F | en |
dc.subject | Sulfonylurea receptor 1 | en |
dc.title | Synthesis and evaluation of 18F-labeled mitiglinide derivatives as positron emission tomography tracers for β-cell imaging. | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.ncid | AA10938083 | - |
dc.identifier.jtitle | Bioorganic & medicinal chemistry | en |
dc.identifier.volume | 22 | - |
dc.identifier.issue | 13 | - |
dc.identifier.spage | 3270 | - |
dc.identifier.epage | 3278 | - |
dc.relation.doi | 10.1016/j.bmc.2014.04.059 | - |
dc.textversion | author | - |
dc.identifier.pmid | 24842616 | - |
dcterms.accessRights | open access | - |
dc.identifier.pissn | 0968-0896 | - |
出現コレクション: | 学術雑誌掲載論文等 |
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