WEKO3
アイテム
{"_buckets": {"deposit": "b9a5a1b7-ddd1-4a9d-8fd0-fe961400cb7a"}, "_deposit": {"created_by": 1, "id": "79840", "owners": [1], "pid": {"revision_id": 0, "type": "depid", "value": "79840"}, "status": "published"}, "_oai": {"id": "oai:repo.qst.go.jp:00079840", "sets": ["1"]}, "author_link": ["1027173", "1027168", "1027174", "1027176", "1027166", "1027177", "1027169", "1027175", "1027161", "1027167", "1027160", "1027170", "1027162", "1027171", "1027172", "1027164", "1027165", "1027163"], "item_8_biblio_info_7": {"attribute_name": "書誌情報", "attribute_value_mlt": [{"bibliographicIssueDates": {"bibliographicIssueDate": "2020-04", "bibliographicIssueDateType": "Issued"}, "bibliographicIssueNumber": "3", "bibliographicPageEnd": "360", "bibliographicPageStart": "353", "bibliographicVolumeNumber": "373", "bibliographic_titles": [{"bibliographic_title": "The Journal of Pharmacology and Experimental Therapeutics"}]}]}, "item_8_description_5": {"attribute_name": "抄録", "attribute_value_mlt": [{"subitem_description": "Fatty acid amide hydrolase (FAAH) is a key enzyme in the endocannabinoid system. N-(3,4-Dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC) was developed as an irreversible-type positron emission tomography (PET) ligand for FAAH. Here, we attempted to noninvasively estimate rate constant k3 as a direct index for FAAH in the rat brain. First, the two-tissue compartment model analysis including three parameters (K1–k3, 2TCMi) in PET study with [11C]DFMC was conducted, which provided 0.21 ± 0.04 mL·cm−3·min−1 of the net uptake value (Ki), an indirect index for FAAH, in the FAAH-richest region (the cingulate cortex). Subsequently, to noninvasively estimate Ki value, the reference model analysis (Patlak Reference, PGAREF) was tried using a time-activity curve of the spinal cord. In that result, the noninvasive Ki value (KREF) was concisely estimated with high correlation (r \u003e 0.95) to Ki values based on 2TCMi. Using estimated KREF value, we tried to obtain calculated-k3 based on previously defined equations. The caluculated-k3 was successfully estimated with high correlation (r = 0.95) to direct k3 in 2TCMi. Finally, the dose relationship study using calculated-k3 demonstrated that in vivo ED50 value of URB597, a major inhibitor of FAAH, was 66.4 µg/kg in rat brain. In conclusion, we proposed the calculated-k3 as an alternative index corresponding to regional FAAH concentrations and suggested that PET with [11C]DFMC enables occupancy study for new pharmaceuticals targeting FAAH.", "subitem_description_type": "Abstract"}]}, "item_8_publisher_8": {"attribute_name": "出版者", "attribute_value_mlt": [{"subitem_publisher": "ASPET"}]}, "item_8_relation_14": {"attribute_name": "DOI", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "10.1124/jpet.119.263772", "subitem_relation_type_select": "DOI"}}]}, "item_8_relation_17": {"attribute_name": "関連サイト", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "https://pubmed.ncbi.nlm.nih.gov/32241809/", "subitem_relation_type_select": "URI"}}]}, "item_8_source_id_9": {"attribute_name": "ISSN", "attribute_value_mlt": [{"subitem_source_identifier": "0022-3565", "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": "Yamasaki, Tomoteru"}], "nameIdentifiers": [{"nameIdentifier": "1027160", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ohya, Tomoyuki"}], "nameIdentifiers": [{"nameIdentifier": "1027161", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Mori, Wakana"}], "nameIdentifiers": [{"nameIdentifier": "1027162", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Yiding"}], "nameIdentifiers": [{"nameIdentifier": "1027163", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Wakizaka, Hidekatsu"}], "nameIdentifiers": [{"nameIdentifier": "1027164", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Nengaki, Nobuki"}], "nameIdentifiers": [{"nameIdentifier": "1027165", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fujinaga, Masayuki"}], "nameIdentifiers": [{"nameIdentifier": "1027166", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kikuchi, Tatsuya"}], "nameIdentifiers": [{"nameIdentifier": "1027167", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ming-Rong, Zhang"}], "nameIdentifiers": [{"nameIdentifier": "1027168", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Tomoteru, Yamasaki", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027169", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Tomoyuki, Ohya", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027170", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Wakana, Mori", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027171", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Yiding", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027172", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Hidekatsu, Wakizaka", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027173", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Nobuki, Nengaki", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027174", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Masayuki, Fujinaga", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027175", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Tatsuya, Kikuchi", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027176", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Ming-Rong", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "1027177", "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": "Development of an In Vivo Method to Estimate Effective Drug Doses and Quantify Fatty Acid Amide Hydrolase in Rodent Brain using Positron Emission Tomography Tracer N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC)", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "Development of an In Vivo Method to Estimate Effective Drug Doses and Quantify Fatty Acid Amide Hydrolase in Rodent Brain using Positron Emission Tomography Tracer N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC)"}]}, "item_type_id": "8", "owner": "1", "path": ["1"], "permalink_uri": "https://repo.qst.go.jp/records/79840", "pubdate": {"attribute_name": "公開日", "attribute_value": "2020-04-10"}, "publish_date": "2020-04-10", "publish_status": "0", "recid": "79840", "relation": {}, "relation_version_is_last": true, "title": ["Development of an In Vivo Method to Estimate Effective Drug Doses and Quantify Fatty Acid Amide Hydrolase in Rodent Brain using Positron Emission Tomography Tracer N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC)"], "weko_shared_id": -1}
Development of an In Vivo Method to Estimate Effective Drug Doses and Quantify Fatty Acid Amide Hydrolase in Rodent Brain using Positron Emission Tomography Tracer N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC)
https://repo.qst.go.jp/records/79840
https://repo.qst.go.jp/records/798404bcd262a-79a8-4ddb-9af6-1675fb002054
Item type | 学術雑誌論文 / Journal Article(1) | |||||
---|---|---|---|---|---|---|
公開日 | 2020-04-10 | |||||
タイトル | ||||||
タイトル | Development of an In Vivo Method to Estimate Effective Drug Doses and Quantify Fatty Acid Amide Hydrolase in Rodent Brain using Positron Emission Tomography Tracer N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC) | |||||
言語 | ||||||
言語 | eng | |||||
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 | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
著者 |
Yamasaki, Tomoteru
× Yamasaki, Tomoteru× Ohya, Tomoyuki× Mori, Wakana× Zhang, Yiding× Wakizaka, Hidekatsu× Nengaki, Nobuki× Fujinaga, Masayuki× Kikuchi, Tatsuya× Ming-Rong, Zhang× Tomoteru, Yamasaki× Tomoyuki, Ohya× Wakana, Mori× Zhang, Yiding× Hidekatsu, Wakizaka× Nobuki, Nengaki× Masayuki, Fujinaga× Tatsuya, Kikuchi× Zhang, Ming-Rong |
|||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Fatty acid amide hydrolase (FAAH) is a key enzyme in the endocannabinoid system. N-(3,4-Dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro-4-[11C]methylphenyl)thiazol-2-yl]-1-carboxamide ([11C]DFMC) was developed as an irreversible-type positron emission tomography (PET) ligand for FAAH. Here, we attempted to noninvasively estimate rate constant k3 as a direct index for FAAH in the rat brain. First, the two-tissue compartment model analysis including three parameters (K1–k3, 2TCMi) in PET study with [11C]DFMC was conducted, which provided 0.21 ± 0.04 mL·cm−3·min−1 of the net uptake value (Ki), an indirect index for FAAH, in the FAAH-richest region (the cingulate cortex). Subsequently, to noninvasively estimate Ki value, the reference model analysis (Patlak Reference, PGAREF) was tried using a time-activity curve of the spinal cord. In that result, the noninvasive Ki value (KREF) was concisely estimated with high correlation (r > 0.95) to Ki values based on 2TCMi. Using estimated KREF value, we tried to obtain calculated-k3 based on previously defined equations. The caluculated-k3 was successfully estimated with high correlation (r = 0.95) to direct k3 in 2TCMi. Finally, the dose relationship study using calculated-k3 demonstrated that in vivo ED50 value of URB597, a major inhibitor of FAAH, was 66.4 µg/kg in rat brain. In conclusion, we proposed the calculated-k3 as an alternative index corresponding to regional FAAH concentrations and suggested that PET with [11C]DFMC enables occupancy study for new pharmaceuticals targeting FAAH. | |||||
書誌情報 |
The Journal of Pharmacology and Experimental Therapeutics 巻 373, 号 3, p. 353-360, 発行日 2020-04 |
|||||
出版者 | ||||||
出版者 | ASPET | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0022-3565 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1124/jpet.119.263772 | |||||
関連サイト | ||||||
識別子タイプ | URI | |||||
関連識別子 | https://pubmed.ncbi.nlm.nih.gov/32241809/ |