{"created":"2023-05-15T14:36:32.529386+00:00","id":47064,"links":{},"metadata":{"_buckets":{"deposit":"eb06c993-0905-4f17-b475-d0152cd32da6"},"_deposit":{"created_by":1,"id":"47064","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"47064"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00047064","sets":["1"]},"author_link":["469992","469994","469981","469977","469982","469974","469989","469976","469995","469986","469984","469983","469985","469988","469987","469990","469980","469975","469973","469991","469996","469979","469978","469993"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2015-02","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"25","bibliographicPageEnd":"19759","bibliographicPageStart":"19752","bibliographicVolumeNumber":"5","bibliographic_titles":[{"bibliographic_title":"RSC Advances"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"The 5-HT7 receptor is a recently cloned G-protein-coupled receptor (GPCR) that is important in regulating\nsleep, depression, and circadian rhythms. However, the potential pathophysiological roles of 5-HT7 have\nnot been fully elucidated, and no 5-HT7 positron emission tomography (PET) radioligands are available,\nthus limiting imaging studies of this receptor in humans. Here, we present the radiosynthesis and\nbiological evaluation of 5-(4-([11C]methoxyphenyl)-1-methyl-4-nitro-1H-imidazole ([11C]1) as a new PET\nligand for 5-HT7. Three-dimensional pharmacophore evaluation and docking studies confirmed its high\naffinity for 5-HT7, and in vitro binding assays showed that the binding affinity was 16.8   0.9 nM. The\nspecific activity was found to be 48   29 GBq mmol 1 for [11C]1 in a synthetic time of 26   3 min (n ¼ 8),\nhaving 38   7% radiochemical yield (decay-corrected) based on [11C]CO2. Ligand interactions with\nhuman serum albumin were studied by fluorescence quenching to obtain a Stern–Volmer plot, which\nshowed a binding constant of 1.15   104 M 1. Whole-body biodistribution patterns were evaluated in\nnormal mice by 1 h dynamic PET imaging; this analysis showed rapid clearance of radioactivity from the\nmain peripheral organs, with the exception of the liver. Preliminary PET studies in rat brains showed rapid\naccumulation of radioactivity in the brain. The regional radioactivity reached a maximum within 0–2 min\nafter the radioligand injection and then decreased rapidly, resulting in minimal radiation burden in the\nbrain during the scan. In summary, this specific biaryl system has shown potential as a 5-HT7 ligand and\nfurther optimization and longitudinal studies may yield the first small molecule-based PET ligand for\n5-HT7 in clinical settings.","subitem_description_type":"Abstract"}]},"item_access_right":{"attribute_name":"アクセス権","attribute_value_mlt":[{"subitem_access_right":"metadata only access","subitem_access_right_uri":"http://purl.org/coar/access_right/c_14cb"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"Tiwari, Anjani"}],"nameIdentifiers":[{"nameIdentifier":"469973","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yui, Joji"}],"nameIdentifiers":[{"nameIdentifier":"469974","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Pooja, Singh"}],"nameIdentifiers":[{"nameIdentifier":"469975","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Agrawal, Swati"}],"nameIdentifiers":[{"nameIdentifier":"469976","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"469977","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"469978","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Chadha, Nidhi"}],"nameIdentifiers":[{"nameIdentifier":"469979","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"469980","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"469981","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shimoda, Yoko"}],"nameIdentifiers":[{"nameIdentifier":"469982","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"469983","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Anil, K Mishra"}],"nameIdentifiers":[{"nameIdentifier":"469984","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"469985","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"469986","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"ティワリ アンジャニ","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469987","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"由井 譲二","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469988","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山崎 友照","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469989","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"謝 琳","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469990","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 一鼎","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469991","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤永 雅之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469992","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"下田 陽子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469993","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"熊田 勝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469994","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"小川 政直","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469995","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"469996","nameIdentifierScheme":"WEKO"}]}]},"item_language":{"attribute_name":"言語","attribute_value_mlt":[{"subitem_language":"eng"}]},"item_resource_type":{"attribute_name":"資源タイプ","attribute_value_mlt":[{"resourcetype":"journal article","resourceuri":"http://purl.org/coar/resource_type/c_6501"}]},"item_title":" Design, synthesis and biological evaluation of small molecule based PET radioligand for 5-HT7 receptor","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":" Design, synthesis and biological evaluation of small molecule based PET radioligand for 5-HT7 receptor"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2015-03-25"},"publish_date":"2015-03-25","publish_status":"0","recid":"47064","relation_version_is_last":true,"title":[" Design, synthesis and biological evaluation of small molecule based PET radioligand for 5-HT7 receptor"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:44:20.970019+00:00"}