{"created":"2023-05-15T16:38:33.829681+00:00","id":12265,"links":{},"metadata":{"_buckets":{"deposit":"ceab1867-5df6-4e38-8fdb-7985a96c4a0a"},"_deposit":{"created_by":2,"id":"12265","owners":[2],"pid":{"revision_id":0,"type":"depid","value":"12265"},"status":"published"},"_oai":{"id":"oai:nagasaki-u.repo.nii.ac.jp:00012265","sets":["73:74"]},"author_link":["45788","45791","45789","45787","45790"],"item_2_biblio_info_6":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2011-11-01","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"21","bibliographicPageEnd":"6253","bibliographicPageStart":"6245","bibliographicVolumeNumber":"19","bibliographic_titles":[{"bibliographic_title":"Bioorganic & Medicinal Chemistry"}]}]},"item_2_description_4":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"In this study, 2-iodo substituted 1-methylpiperidin-2-yl benzamide derivatives were synthesized and evaluated as candidate SPECT imaging agents for glycine transporter 1 (GlyT1). In JAR cells, which predominantly express GlyT1, 2-iodo N-[(S)-{(S)-1-methylpiperidin-2-yl}(phenyl)methyl]3-trifluoromethyl-benzamide (5) showed excellent inhibitory activity of [(3)H]glycine uptake (IC(50)=2.4nM). Saturation assay in rat cortical membranes revealed that [(125)I]5 had a single high affinity binding site with a K(d) of 1.54nM and a B(max) of 3.40pmol/mg protein. In vitro autoradiography demonstrated that [(125)I]5 showed consistent accumulation with GlyT1 expression. The in vitro binding was greatly inhibited by GlyT1 inhibitors but not by other site ligands, which suggested the high specific binding of [(125)I]5 with GlyT1. In the biodistribution and ex vivo autoradiography studies using mice, [(125)I]5 showed high blood-brain barrier permeability (1.68-2.17% dose/g at 15-60min) and similar regional brain distribution pattern with in vitro results. In addition, pre-treatment of GlyT1 ligands resulted in significant decrease of [(125)I]5 binding in the GlyT1-rich regions. This preliminary study demonstrated that radio-iodinated 5 is a promising SPECT imaging probe for GlyT1.","subitem_description_type":"Abstract"}]},"item_2_description_63":{"attribute_name":"引用","attribute_value_mlt":[{"subitem_description":"Bioorganic & Medicinal Chemistry, 19(21), pp.6245-6253; 2011","subitem_description_type":"Other"}]},"item_2_publisher_33":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Elsevier BV"}]},"item_2_relation_11":{"attribute_name":"PubMed番号","attribute_value_mlt":[{"subitem_relation_type":"isVersionOf","subitem_relation_type_id":{"subitem_relation_type_id_text":"21975065","subitem_relation_type_select":"PMID"}}]},"item_2_relation_12":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type":"isVersionOf","subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1016/j.bmc.2011.09.010","subitem_relation_type_select":"DOI"}}]},"item_2_rights_13":{"attribute_name":"権利","attribute_value_mlt":[{"subitem_rights":"Copyright © 2011 Elsevier Ltd. All rights reserved."}]},"item_2_source_id_10":{"attribute_name":"書誌レコードID","attribute_value_mlt":[{"subitem_source_identifier":"AA10938083","subitem_source_identifier_type":"NCID"}]},"item_2_source_id_7":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"09680896","subitem_source_identifier_type":"ISSN"}]},"item_2_source_id_8":{"attribute_name":"EISSN","attribute_value_mlt":[{"subitem_source_identifier":"14643391","subitem_source_identifier_type":"ISSN"}]},"item_2_version_type_16":{"attribute_name":"著者版フラグ","attribute_value_mlt":[{"subitem_version_resource":"http://purl.org/coar/version/c_ab4af688f83e57aa","subitem_version_type":"AM"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"Fuchigami, Takeshi"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Haratake, Mamoru"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Magata, Yasuhiro"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Haradahira, Terushi"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"Nakayama, Morio"}],"nameIdentifiers":[{}]}]},"item_files":{"attribute_name":"ファイル情報","attribute_type":"file","attribute_value_mlt":[{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2020-12-22"}],"displaytype":"detail","filename":"BMC19_6245.pdf","filesize":[{"value":"1.0 MB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"BMC19_6245.pdf","url":"https://nagasaki-u.repo.nii.ac.jp/record/12265/files/BMC19_6245.pdf"},"version_id":"9d4fd504-1588-4e2b-b561-5915790f0a7d"}]},"item_keyword":{"attribute_name":"キーワード","attribute_value_mlt":[{"subitem_subject":"125I","subitem_subject_scheme":"Other"},{"subitem_subject":"glycine transporter 1 (GlyT1)","subitem_subject_scheme":"Other"},{"subitem_subject":"schizophrenia","subitem_subject_scheme":"Other"},{"subitem_subject":"Single photon emission computed","subitem_subject_scheme":"Other"},{"subitem_subject":"tomography (SPECT)","subitem_subject_scheme":"Other"}]},"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":"Synthesis and characterization of [(125)I]2-iodo N-[(S)-{(S)-1-methylpiperidin-2-yl}(phenyl)methyl]3-trifluoromethyl-benzamide as novel imaging probe for glycine transporter 1.","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Synthesis and characterization of [(125)I]2-iodo N-[(S)-{(S)-1-methylpiperidin-2-yl}(phenyl)methyl]3-trifluoromethyl-benzamide as novel imaging probe for glycine transporter 1."}]},"item_type_id":"2","owner":"2","path":["74"],"pubdate":{"attribute_name":"公開日","attribute_value":"2011-11-15"},"publish_date":"2011-11-15","publish_status":"0","recid":"12265","relation_version_is_last":true,"title":["Synthesis and characterization of [(125)I]2-iodo N-[(S)-{(S)-1-methylpiperidin-2-yl}(phenyl)methyl]3-trifluoromethyl-benzamide as novel imaging probe for glycine transporter 1."],"weko_creator_id":"2","weko_shared_id":2},"updated":"2023-05-15T18:52:26.978282+00:00"}