WEKO3
アイテム
{"_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": ["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 \u0026 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 \u0026 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": [{"nameIdentifier": "45787", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Haratake, Mamoru"}], "nameIdentifiers": [{"nameIdentifier": "45788", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Magata, Yasuhiro"}], "nameIdentifiers": [{"nameIdentifier": "45789", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Haradahira, Terushi"}], "nameIdentifiers": [{"nameIdentifier": "45790", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Nakayama, Morio"}], "nameIdentifiers": [{"nameIdentifier": "45791", "nameIdentifierScheme": "WEKO"}]}]}, "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", "download_preview_message": "", "file_order": 0, "filename": "BMC19_6245.pdf", "filesize": [{"value": "1.0 MB"}], "format": "application/pdf", "future_date_message": "", "is_thumbnail": false, "licensetype": "license_free", "mimetype": "application/pdf", "size": 1000000.0, "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"], "permalink_uri": "http://hdl.handle.net/10069/26394", "pubdate": {"attribute_name": "公開日", "attribute_value": "2011-11-15"}, "publish_date": "2011-11-15", "publish_status": "0", "recid": "12265", "relation": {}, "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_shared_id": 2}
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.
http://hdl.handle.net/10069/26394
http://hdl.handle.net/10069/2639499f2000b-e840-439d-80e6-de0e32488e84
名前 / ファイル | ライセンス | アクション |
---|---|---|
BMC19_6245.pdf (1.0 MB)
|
|
Item type | 学術雑誌論文 / Journal Article(1) | |||||
---|---|---|---|---|---|---|
公開日 | 2011-11-15 | |||||
タイトル | ||||||
タイトル | 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. | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | 125I | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | glycine transporter 1 (GlyT1) | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | schizophrenia | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Single photon emission computed | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | tomography (SPECT) | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
Fuchigami, Takeshi
× Fuchigami, Takeshi× Haratake, Mamoru× Magata, Yasuhiro× Haradahira, Terushi× Nakayama, Morio |
|||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | 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. | |||||
書誌情報 |
Bioorganic & Medicinal Chemistry 巻 19, 号 21, p. 6245-6253, 発行日 2011-11-01 |
|||||
出版者 | ||||||
出版者 | Elsevier BV | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 09680896 | |||||
EISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 14643391 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA10938083 | |||||
PubMed番号 | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | PMID | |||||
関連識別子 | 21975065 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.bmc.2011.09.010 | |||||
権利 | ||||||
権利情報 | Copyright © 2011 Elsevier Ltd. All rights reserved. | |||||
著者版フラグ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
引用 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Bioorganic & Medicinal Chemistry, 19(21), pp.6245-6253; 2011 |