{"created":"2023-05-15T16:30:27.024309+00:00","id":1581,"links":{},"metadata":{"_buckets":{"deposit":"b5dd8ffc-a6a1-4e2f-8f17-02beb2c17a13"},"_deposit":{"created_by":2,"id":"1581","owners":[2],"pid":{"revision_id":0,"type":"depid","value":"1581"},"status":"published"},"_oai":{"id":"oai:nagasaki-u.repo.nii.ac.jp:00001581","sets":["73:74"]},"author_link":["7611","7612","7614","7617","7615","7613","7609","7616","7610","7608"],"item_2_biblio_info_6":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"1991","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"2","bibliographicPageEnd":"105","bibliographicPageStart":"101","bibliographicVolumeNumber":"14","bibliographic_titles":[{"bibliographic_title":"Journal of Pharmacobio-Dynamics"}]}]},"item_2_description_4":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"The opioid activity and the selectivity for opioid receptor (subtypes) of newly synthesized fluorinated enkephalin (Enk) analogues, [2R, 4R], [2R, 4S], [2S, 4S] and [2S, 4R] trifluoro-Leu5-Enk (KKF-31, 32, 33 and 34) were investigated. The inhibitory effect of KKF-compounds on the electrically induced contractions of guinea-pig ileum (GPI) and mouse vas deferens (MVD) were dosedependent but relatively lower than that of L-Leu5-Enk, except that KKF-34 was rather slightly more potent than L-Leu5-Enk in MVD preparations. In GPI preparations, the pA2 values of naloxone for these compounds were higher than those of naltrindole while the values of naltrindole for KKF-compound were higher than those of naloxone in MVD preparations. Intracerebroventricular KKF-31 and KKF-32 at doses of 20 and 10 nmol/mouse, respectively, produced analgesia comparable to 0.1 nmol Tyr-D-Arg-Phe-Lys-NH2 and 100 nmol Tyr-D-Thr-Gly-Phe-Leu-Thr; however, neither KKF-33 nor 34 produced analgesia up to the doses of 100 nmol/mouse. Both naloxone, 1 mg/kg, i.p., and naltrindole, 10 mg/kg, i.p., antagonized KKF-31- and KKF-32-induced analgesia. The results suggest that the introduction of trifluoromethyl group in Leu5 results in the alternation of the opioid activity and receptor selectivity. Although KKF-33 and KKF-34 possessed a more potent in vitro inhibitory effect than KKF-31 and KKF-32, mediated through μ- and δ-opioid receptors in both preparations, they did not show any appreciable analgesic effect. KKF-31 and KKF-32 produce naloxone-and naltrindole-reversible analgesia irrespective of in vitro μ- and δ-opioid activity.","subitem_description_type":"Abstract"}]},"item_2_description_63":{"attribute_name":"引用","attribute_value_mlt":[{"subitem_description":"Journal of Pharmacobio-Dynamics, 14(2), pp.101-105; 1991","subitem_description_type":"Other"}]},"item_2_publisher_33":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"日本薬学会"}]},"item_2_relation_12":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type":"isIdenticalTo","subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1248/bpb1978.14.101","subitem_relation_type_select":"DOI"}}]},"item_2_rights_13":{"attribute_name":"権利","attribute_value_mlt":[{"subitem_rights":"c The Pharmaceutical Society of Japan"}]},"item_2_source_id_10":{"attribute_name":"書誌レコードID","attribute_value_mlt":[{"subitem_source_identifier":"AA00704585","subitem_source_identifier_type":"NCID"}]},"item_2_source_id_7":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0386846X","subitem_source_identifier_type":"ISSN"}]},"item_2_source_id_8":{"attribute_name":"EISSN","attribute_value_mlt":[{"subitem_source_identifier":"18811353","subitem_source_identifier_type":"ISSN"}]},"item_2_text_62":{"attribute_name":"出版者別言語","attribute_value_mlt":[{"subitem_text_value":"Pharmaceutical Society of Japan"}]},"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_970fb48d4fbd8a85","subitem_version_type":"VoR"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"WATANABE, Joe"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"TOKUYAMA, Shogo"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"TAKAHASHI, Masakatsu"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"KANETO, Hiroshi"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"MAEDA, Mitsuko"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"KAWASAKI, Koichi"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"TAGUCHI, Takeo"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"KOBAYASHI, Yoshiro"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"YAMAMOTO, Yoshihiro"}],"nameIdentifiers":[{}]},{"creatorNames":[{"creatorName":"SHIMOKAWA, Kazuhiro"}],"nameIdentifiers":[{}]}]},"item_files":{"attribute_name":"ファイル情報","attribute_type":"file","attribute_value_mlt":[{"accessrole":"open_date","date":[{"dateType":"Available","dateValue":"2020-12-18"}],"displaytype":"detail","filename":"JPD14_101.pdf","filesize":[{"value":"601.1 kB"}],"format":"application/pdf","licensetype":"license_note","mimetype":"application/pdf","url":{"label":"JPD14_101.pdf","url":"https://nagasaki-u.repo.nii.ac.jp/record/1581/files/JPD14_101.pdf"},"version_id":"2c199b4b-0815-4856-939a-74277c626230"}]},"item_keyword":{"attribute_name":"キーワード","attribute_value_mlt":[{"subitem_subject":"naltrindole","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":"The opioid activity and receptor selectivity of fluorinated Leu5 Enkephalin analogues in vitro and in vivo.","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"The opioid activity and receptor selectivity of fluorinated Leu5 Enkephalin analogues in vitro and in vivo."}]},"item_type_id":"2","owner":"2","path":["74"],"pubdate":{"attribute_name":"公開日","attribute_value":"2019-02-21"},"publish_date":"2019-02-21","publish_status":"0","recid":"1581","relation_version_is_last":true,"title":["The opioid activity and receptor selectivity of fluorinated Leu5 Enkephalin analogues in vitro and in vivo."],"weko_creator_id":"2","weko_shared_id":-1},"updated":"2023-05-16T03:59:53.352313+00:00"}