pubmed-article:21482120 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0031268 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C1257954 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0538927 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0220825 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0870883 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0032743 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0182400 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C0205164 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
pubmed-article:21482120 | lifeskim:mentions | umls-concept:C1705294 | lld:lifeskim |
pubmed-article:21482120 | pubmed:issue | 9 | lld:pubmed |
pubmed-article:21482120 | pubmed:dateCreated | 2011-4-28 | lld:pubmed |
pubmed-article:21482120 | pubmed:abstractText | Synthesis of [(11)C]celecoxib, a selective COX-2 inhibitor, and [(11)C]SC-62807, a major metabolite of celecoxib, were achieved and the potential of these PET probes for assessing the function of drug transporter in biliary excretion was evaluated. The synthesis of [(11)C]celecoxib was achieved in one-pot by reacting [(11)C]methyl iodide with an excess of the corresponding pinacol borate precursor using Pd(2)(dba)(3), P(o-tolyl)(3), and K(2)CO(3) (1:4:9) in DMF. The radiochemical yield of [(11)C]celecoxib was 63±23% (decay-corrected, based on [(11)C]CH(3)I) (n=7) with a specific radioactivity of 83±23GBq/?mol (n=7). The average time of synthesis from end of bombardment including formulation was 30min with >99% radiochemical purity. [(11)C]SC-62807 was synthesized from [(11)C]celecoxib by further rapid oxidation in the presence of excess KMnO(4) with microwave irradiation. The radiochemical yield of [(11)C]SC-62807 was 55±9% (n=3) (decay-corrected, based on [(11)C]celecoxib) with a specific radioactivity of 39±4GBq/?mol (n=3). The average time of synthesis from [(11)C]celecoxib including formulation was 20min and the radiochemical purity was >99%. PET studies in rats and the metabolite analyzes of [(11)C]celecoxib and [(11)C]SC-62807 showed largely different excretion processes, and consequently, [(11)C]SC-62807 was rapidly excreted via hepatobiliary excretion without further metabolism. [(11)C]SC-62807 was shown to have a high potential as a PET probe for evaluating drug transporter function in biliary excretion. | lld:pubmed |
pubmed-article:21482120 | pubmed:language | eng | lld:pubmed |
pubmed-article:21482120 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:21482120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21482120 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:21482120 | pubmed:month | May | lld:pubmed |
pubmed-article:21482120 | pubmed:issn | 1464-3391 | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:SugiyamaYuich... | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:WatanabeYasuy... | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:SuzukiMasaaki... | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:TakashimaTada... | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:WadaYasuhiroY | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:DoiHisashiH | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:KatayamaYumik... | lld:pubmed |
pubmed-article:21482120 | pubmed:author | pubmed-author:Takashima-Hir... | lld:pubmed |
pubmed-article:21482120 | pubmed:copyrightInfo | Copyright © 2011 Elsevier Ltd. All rights reserved. | lld:pubmed |
pubmed-article:21482120 | pubmed:issnType | Electronic | lld:pubmed |
pubmed-article:21482120 | pubmed:day | 1 | lld:pubmed |
pubmed-article:21482120 | pubmed:volume | 19 | lld:pubmed |
pubmed-article:21482120 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:21482120 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:21482120 | pubmed:pagination | 2997-3004 | lld:pubmed |
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pubmed-article:21482120 | pubmed:year | 2011 | lld:pubmed |
pubmed-article:21482120 | pubmed:articleTitle | Efficient sequential synthesis of PET Probes of the COX-2 inhibitor [11C]celecoxib and its major metabolite [11C]SC-62807 and in vivo PET evaluation. | lld:pubmed |
pubmed-article:21482120 | pubmed:affiliation | RIKEN Center for Molecular Imaging Science, Kobe, Japan. | lld:pubmed |
pubmed-article:21482120 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:21482120 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:21482120 | lld:chembl |