{"created":"2023-06-20T16:59:53.636348+00:00","id":19114,"links":{},"metadata":{"_buckets":{"deposit":"944e258a-5b06-4f3c-a074-084f4e5a3e4f"},"_deposit":{"created_by":3,"id":"19114","owners":[3],"pid":{"revision_id":0,"type":"depid","value":"19114"},"status":"published"},"_oai":{"id":"oai:twinkle.repo.nii.ac.jp:00019114","sets":["140:1307:1308:1984:1985"]},"author_link":["298084","298083","298086","298085"],"item_10001_alternative_title_1":{"attribute_name":"別タイトル","attribute_value_mlt":[{"subitem_alternative_title":"新規1,4ベンゾチアゼピン誘導体K201のラット大動脈平滑筋の細胞内Caと収縮への効果"}]},"item_10001_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2004-01","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"1","bibliographicPageEnd":"46","bibliographicPageStart":"39","bibliographicVolumeNumber":"74","bibliographic_titles":[{"bibliographic_title":"東京女子医科大学雑誌"}]}]},"item_10001_creator_2":{"attribute_name":"著者名","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"SHIMAMOTO, Ken"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"KANEKO, Noboru"}],"nameIdentifiers":[{}]}]},"item_10001_date_25":{"attribute_name":"受付日付","attribute_value_mlt":[{"subitem_date_issued_datetime":"2010-08-10","subitem_date_issued_type":"Created"}]},"item_10001_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"1,4ベンゾチアゼピン誘導体K201 (JTV519)は心筋保護を目的に新規合成された.心筋ではナトリウム,カリウム,カルシウムチャンネルの阻害作用があり,抗虚血,抗不整脈作用を有する.この研究ではラット大動脈を用いて, K201の平滑筋の細胞内カルシウムと収縮への作用を検討した.細胞内カルシウム測定には蛍光指示薬furaPE3/AMと放射性カルシウム45(45 Ca)を用いた.カルシウム除去液では, 10-6Mノルエピネフリンによる収縮は持続性であるが,カルシウムトランジエント([Ca2+]i)は一過性であった.この収縮と[Ca2+]iは10-5M K201の前投与により消失した. 72.7mM高濃度カリウムによる収縮を10-5>M K201は100%抑制するが, [Ca2+]iは約20%が残存した.この残存した[Ca2+]iは10-5Mベラパミルで消失した.高濃度カリウムによる脱分極では, 10-4M K201の前投与による^<45>Caの流入の抑制は34%で, 10-5Mジルチアゼムによる抑制は85%であった. 10-4M K201と10-5Mジルチアゼムはほぼ完全に高濃度カリウムによる収縮を抑制した. K201の血管平滑筋収縮抑制への作用機序としてCaチャンネル拮抗作用,α受容体阻害作用では十分に説明できず, Ca感受性を変える細胞内Ca拮抗作用が推測される.","subitem_description_type":"Abstract"},{"subitem_description":"The 1,4-benzothiazepine derivative K201 (synonym JTV519) was newly synthesized for use as a cardioprotective agent. This study was conducted to examine the effects of K201 on rat aortic smooth muscle contraction and the mobilization of intracellular Ca2+. Intracellular Ca2+ level was determined using a fluorescent Ca2+ indicator furaPE3 and 45Ca2+. Norepinephrine induced transient contraction and an increase in calcium transient ([Ca2+]i) under Ca2+-free conditions in isolated rat aorta smooth muscle samples. Pretreatment with K201 at 10-5 M inhibited the contraction and increase of [Ca2+]i induced by norepinephrine at 10-6 M. K201 at 10-5 M almost completely inhibited the vascular smooth muscle contraction induced by high potassium (K+), although approximately 20% of calcium transient remained. Addition of 10-5 M verapamil almost completely inhibited the resting [Ca2+]i. [Ca2+]i-tension relationship was examined at various doses of K201 and diltiazem in rat aorta stimulated by high K+. Both muscle tension and [Ca2+]i decreased by K201 dose-dependently, greater relaxation was induced by K201 than by diltiazem at the same resting level of [Ca2+]i. In high K+-induced depolarization, pretreatment with K201 at 10-4 M inhibited 45 Ca2+ influx by 34%, while diltiazem at 10-5 M inhibited the influx by 85%. In addition to a mild α-adrenoceptor and Ca2+ -channel blocking activity, K201 may alter the Ca2+ sensitivity of intracellular contractile elements.","subitem_description_type":"Abstract"}]},"item_10001_full_name_3":{"attribute_name":"著者別名","attribute_value_mlt":[{"nameIdentifiers":[{"nameIdentifier":"298085","nameIdentifierScheme":"WEKO"}],"names":[{"name":"島本, 健"}]},{"nameIdentifiers":[{"nameIdentifier":"298086","nameIdentifierScheme":"WEKO"}],"names":[{"name":"金子, 昇"}]}]},"item_10001_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"東京女子医科大学学会"}]},"item_10001_source_id_11":{"attribute_name":"NCID","attribute_value_mlt":[{"subitem_source_identifier":"AN00161368","subitem_source_identifier_type":"NCID"}]},"item_10001_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0040-9022","subitem_source_identifier_type":"ISSN"}]},"item_10001_subject_47":{"attribute_name":"著者キーワード","attribute_value_mlt":[{"subitem_subject":"K201 (JTV519)","subitem_subject_scheme":"Other"},{"subitem_subject":"Ca2+-channel blocker","subitem_subject_scheme":"Other"},{"subitem_subject":"Ca2+ sensitivity","subitem_subject_scheme":"Other"},{"subitem_subject":"smooth muscle","subitem_subject_scheme":"Other"},{"subitem_subject":"furaPE3","subitem_subject_scheme":"Other"},{"subitem_subject":"AM","subitem_subject_scheme":"Other"}]},"item_10001_text_35":{"attribute_name":"著者所属","attribute_value_mlt":[{"subitem_text_value":"Department of Cardiology, Tokyo Women's Medical University Aoyama Hospital"},{"subitem_text_value":"Department of Cardiology and Pneumology, Dokkyo University School of Medicine"},{"subitem_text_value":"東京女子医科大学附属青山病院循環器内科"},{"subitem_text_value":"獨協医科大学心血管肺内科"}]},"item_10001_version_type_20":{"attribute_name":"著者版フラグ","attribute_value_mlt":[{"subitem_version_resource":"http://purl.org/coar/version/c_970fb48d4fbd8a85","subitem_version_type":"VoR"}]},"item_files":{"attribute_name":"ファイル情報","attribute_type":"file","attribute_value_mlt":[{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2017-08-22"}],"displaytype":"detail","filename":"KJ00006018689.pdf","filesize":[{"value":"794.4 kB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"KJ00006018689.pdf","url":"https://twinkle.repo.nii.ac.jp/record/19114/files/KJ00006018689.pdf"},"version_id":"161184d0-74d1-46ee-831f-030b7a0a6fd5"}]},"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":"Effects of a Novel 1,4-Benzothiazepine Derivative, K201, on Cytosolic Ca2+ and Contraction in Isolated Smooth Muscle of Rat Aorta","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Effects of a Novel 1,4-Benzothiazepine Derivative, K201, on Cytosolic Ca2+ and Contraction in Isolated Smooth Muscle of Rat Aorta"}]},"item_type_id":"10001","owner":"3","path":["1985"],"pubdate":{"attribute_name":"公開日","attribute_value":"2010-08-10"},"publish_date":"2010-08-10","publish_status":"0","recid":"19114","relation_version_is_last":true,"title":["Effects of a Novel 1,4-Benzothiazepine Derivative, K201, on Cytosolic Ca2+ and Contraction in Isolated Smooth Muscle of Rat Aorta"],"weko_creator_id":"3","weko_shared_id":-1},"updated":"2023-06-20T20:57:04.902839+00:00"}