{"created":"2023-05-15T14:36:39.156524+00:00","id":47213,"links":{},"metadata":{"_buckets":{"deposit":"ebfff7c4-6e94-4947-9a79-542d001544ae"},"_deposit":{"created_by":1,"id":"47213","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"47213"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00047213","sets":["1"]},"author_link":["471946","471941","471938","471939","471942","471951","471943","471950","471936","471949","471953","471954","471944","471945","471940","471937","471947","471948","471952"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2010-10","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"20","bibliographicPageEnd":"7355","bibliographicPageStart":"7344","bibliographicVolumeNumber":"53","bibliographic_titles":[{"bibliographic_title":"Journal of medicinal chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Here we describe the design, synthesis, and evaluation of physicochemical and pharmacological properties of D(4) dopamine receptor ligands related to N-[2-[4-(4-chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide (2). Structural features were incorporated to increase affinity for the target receptor, to improve selectivity over D(2) and σ(1) receptors, to enable labeling with carbon-11 or fluorine-18, and to adjust lipophilicity within the range considered optimal for brain penetration and low nonspecific binding. Compounds 7 and 13 showed the overall best characteristics: nanomolar affinity for the D(4) receptor, >100-fold selectivity over D(2) and D(3) dopamine receptors, 5-HT(1A), 5-HT(2A), and 5-HT(2C) serotonin receptors and σ(1) receptors, and log P = 2.37-2.55. Following intraperitoneal administration in mice, both compounds rapidly entered the central nervous system. The methoxy of N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide (7) was radiolabeled with carbon-11 and subjected to PET analysis in non-human primate. [(11)C]7 time-dependently accumulated to saturation in the posterior eye in the region of the retina, a tissue containing a high density of D(4) receptors.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"American Chemical Society"}]},"item_8_relation_13":{"attribute_name":"PubMed番号","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"20873719","subitem_relation_type_select":"PMID"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0022-2623","subitem_source_identifier_type":"ISSN"}]},"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":"Lacivita, Enza"}],"nameIdentifiers":[{"nameIdentifier":"471936","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"De, Giorgio Paola"}],"nameIdentifiers":[{"nameIdentifier":"471937","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"T, Lee Irene"}],"nameIdentifiers":[{"nameIdentifier":"471938","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"I, Rodeheaver Sean"}],"nameIdentifiers":[{"nameIdentifier":"471939","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"A, Weiss Bryan"}],"nameIdentifiers":[{"nameIdentifier":"471940","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fracasso, Claudia"}],"nameIdentifiers":[{"nameIdentifier":"471941","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Caccia, Silvio"}],"nameIdentifiers":[{"nameIdentifier":"471942","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Berardi, Francesco"}],"nameIdentifiers":[{"nameIdentifier":"471943","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Perrone, Roberto"}],"nameIdentifiers":[{"nameIdentifier":"471944","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"471945","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Jun"}],"nameIdentifiers":[{"nameIdentifier":"471946","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Higuchi, Makoto"}],"nameIdentifiers":[{"nameIdentifier":"471947","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suhara, Tetsuya"}],"nameIdentifiers":[{"nameIdentifier":"471948","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"A, Schetz John"}],"nameIdentifiers":[{"nameIdentifier":"471949","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Leopoldo, Marcello"}],"nameIdentifiers":[{"nameIdentifier":"471950","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"471951","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"前田 純","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"471952","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"樋口 真人","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"471953","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"須原 哲也","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"471954","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, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors.","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors."}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2015-08-06"},"publish_date":"2015-08-06","publish_status":"0","recid":"47213","relation_version_is_last":true,"title":["Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors."],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:42:32.160597+00:00"}