ログイン
言語:

WEKO3

  • トップ
  • ランキング
To
lat lon distance
To

Field does not validate



インデックスリンク

インデックスツリー

メールアドレスを入力してください。

WEKO

One fine body…

WEKO

One fine body…

アイテム

{"_buckets": {"deposit": "7ac987e4-ea6d-4c6f-b8ee-9a1cd1c75ca0"}, "_deposit": {"created_by": 1, "id": "72338", "owners": [1], "pid": {"revision_id": 0, "type": "depid", "value": "72338"}, "status": "published"}, "_oai": {"id": "oai:repo.qst.go.jp:00072338", "sets": ["28"]}, "author_link": ["712456", "712461", "712460", "712464", "712468", "712476", "712469", "712475", "712472", "712474", "712454", "712458", "712459", "712473", "712465", "712455", "712471", "712463", "712452", "712462", "712466", "712470", "712453", "712457", "712477", "712467"], "item_10005_date_7": {"attribute_name": "発表年月日", "attribute_value_mlt": [{"subitem_date_issued_datetime": "2017-05-15", "subitem_date_issued_type": "Issued"}]}, "item_10005_description_5": {"attribute_name": "抄録", "attribute_value_mlt": [{"subitem_description": "Objectives: Growth hormone secretagogue receptor 1a (GHS-R1a) is a G protein-coupled receptor and  expressed predominantly in the pituitary gland, at lower levels in the brain regions including hypothalamus that regulate feeding behavior and glucose sensing, and at even lower level in the pancreas. Therefore, GHSR1a is a promising drug target for complex neuroendocrine disorders that involve in both the central nervous system and the endocrine system. Recently, we developed PET probes for imaging of GHS-R1a ([18F]FEGRL1 and [11C]GRL2). These PET probes showed moderate uptake and low specific binding in the brain and pancreas. To improve uptake of radioactivity and specific binding in the brain and pancreas, we searched new candidate agents for a useful PET probe. Among the investigated compounds, (S)-(4-(1H-indole-6-carbonyl)-3-methylpiperazin-1-yl)(4’-methoxy-[1,1’-biphenyl]-4-yl)methanone (GRL3) has a high selective affinity for GHS-R1a (IC50 = 7.0 nmol/L)[1], and is possible for 11C labeling. Thus, we developed [11C]GRL3 as a new PET probe for imaging of GHS-R1a in the brain and pancreas.\nMethods: [11C]GRL3 was synthesized by the methylation of its precursor (1.0 mg) with [11C]methyl iodide in the presence of 0.5 mol/L sodium hydroxide solution (5 μL) at 80ºC for 5 min. Biodistribution studies were conducted in mice.\nResults: In the radiosynthesis, the decay-corrected radiochemical yield from 11CO2 was 43±8% (n = 10) at the end of radionuclide production, the molar radioactivity was 104±64 GBq/μmol (n = 15) at the end of synthesis, the radiochemical purity was \u003e99%, and the synthesis time was approximately 30 min. In the biodistribution, radioactivity level of pancreas was highest (6.5 %ID/g) and that of brain was lowest (0.4 %ID/g) among all investigated tissues at 60 min after the injection. The radioactivity level in pancreas was gradually increased until 30 min after the injection, and maintained for 60 min after the injection. By pretreatment with YIL-781, which has high and selective affinity for GHS-R1a, the radioactivity level of pancreas at 30 min after the injection was significantly reduced to 55% of control, but that of brain was not changed.\nConclusions: [11C]GRL3 was successfully synthesized as an injection, and showed relatively high uptake and specific binding of the pancreas in mice. [11C]GRL3 may be a useful PET probe for imaging of GHS-R1a in the pancreas.", "subitem_description_type": "Abstract"}]}, "item_10005_description_6": {"attribute_name": "会議概要(会議名, 開催地, 会期, 主催者等)", "attribute_value_mlt": [{"subitem_description": "22nd International symposium on radiopharmaceutical science (ISRS)", "subitem_description_type": "Other"}]}, "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": "Kawamura, Kazunori"}], "nameIdentifiers": [{"nameIdentifier": "712452", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fujinaga, Masayuki"}], "nameIdentifiers": [{"nameIdentifier": "712453", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Shimoda, Yoko"}], "nameIdentifiers": [{"nameIdentifier": "712454", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Yamasaki, Tomoteru"}], "nameIdentifiers": [{"nameIdentifier": "712455", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Yiding"}], "nameIdentifiers": [{"nameIdentifier": "712456", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Hatori, Akiko"}], "nameIdentifiers": [{"nameIdentifier": "712457", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Xie, Lin"}], "nameIdentifiers": [{"nameIdentifier": "712458", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Wakizaka, Hidekatsu"}], "nameIdentifiers": [{"nameIdentifier": "712459", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kurihara, Yusuke"}], "nameIdentifiers": [{"nameIdentifier": "712460", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ohkubo, Takayuki"}], "nameIdentifiers": [{"nameIdentifier": "712461", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ogawa, Masanao"}], "nameIdentifiers": [{"nameIdentifier": "712462", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Nengaki, Nobuki"}], "nameIdentifiers": [{"nameIdentifier": "712463", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Ming-Rong"}], "nameIdentifiers": [{"nameIdentifier": "712464", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "河村 和紀", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712465", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "藤永 雅之", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712466", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "下田 陽子", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712467", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "山崎 友照", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712468", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "張 一鼎", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712469", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "羽鳥 晶子", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712470", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "謝 琳", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712471", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "脇坂 秀克", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712472", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "栗原 雄祐", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712473", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "大久保 崇之", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712474", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "小川 政直", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712475", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "念垣 信樹", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712476", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "張 明栄", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "712477", "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": "conference object", "resourceuri": "http://purl.org/coar/resource_type/c_c94f"}]}, "item_title": "Synthesis and evaluation of a new 11C-labeled growth hormone secretagogue receptor 1a probe", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "Synthesis and evaluation of a new 11C-labeled growth hormone secretagogue receptor 1a probe"}]}, "item_type_id": "10005", "owner": "1", "path": ["28"], "permalink_uri": "https://repo.qst.go.jp/records/72338", "pubdate": {"attribute_name": "公開日", "attribute_value": "2017-05-25"}, "publish_date": "2017-05-25", "publish_status": "0", "recid": "72338", "relation": {}, "relation_version_is_last": true, "title": ["Synthesis and evaluation of a new 11C-labeled growth hormone secretagogue receptor 1a probe"], "weko_shared_id": -1}
  1. 学会発表・講演等
  2. ポスター発表

Synthesis and evaluation of a new 11C-labeled growth hormone secretagogue receptor 1a probe

https://repo.qst.go.jp/records/72338
https://repo.qst.go.jp/records/72338
f2bd608f-8c70-437f-ab3c-eff06667ffdb
Item type 会議発表用資料 / Presentation(1)
公開日 2017-05-25
タイトル
タイトル Synthesis and evaluation of a new 11C-labeled growth hormone secretagogue receptor 1a probe
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_c94f
資源タイプ conference object
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 Kawamura, Kazunori

× Kawamura, Kazunori

WEKO 712452

Kawamura, Kazunori

Search repository
Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 712453

Fujinaga, Masayuki

Search repository
Shimoda, Yoko

× Shimoda, Yoko

WEKO 712454

Shimoda, Yoko

Search repository
Yamasaki, Tomoteru

× Yamasaki, Tomoteru

WEKO 712455

Yamasaki, Tomoteru

Search repository
Zhang, Yiding

× Zhang, Yiding

WEKO 712456

Zhang, Yiding

Search repository
Hatori, Akiko

× Hatori, Akiko

WEKO 712457

Hatori, Akiko

Search repository
Xie, Lin

× Xie, Lin

WEKO 712458

Xie, Lin

Search repository
Wakizaka, Hidekatsu

× Wakizaka, Hidekatsu

WEKO 712459

Wakizaka, Hidekatsu

Search repository
Kurihara, Yusuke

× Kurihara, Yusuke

WEKO 712460

Kurihara, Yusuke

Search repository
Ohkubo, Takayuki

× Ohkubo, Takayuki

WEKO 712461

Ohkubo, Takayuki

Search repository
Ogawa, Masanao

× Ogawa, Masanao

WEKO 712462

Ogawa, Masanao

Search repository
Nengaki, Nobuki

× Nengaki, Nobuki

WEKO 712463

Nengaki, Nobuki

Search repository
Zhang, Ming-Rong

× Zhang, Ming-Rong

WEKO 712464

Zhang, Ming-Rong

Search repository
河村 和紀

× 河村 和紀

WEKO 712465

en 河村 和紀

Search repository
藤永 雅之

× 藤永 雅之

WEKO 712466

en 藤永 雅之

Search repository
下田 陽子

× 下田 陽子

WEKO 712467

en 下田 陽子

Search repository
山崎 友照

× 山崎 友照

WEKO 712468

en 山崎 友照

Search repository
張 一鼎

× 張 一鼎

WEKO 712469

en 張 一鼎

Search repository
羽鳥 晶子

× 羽鳥 晶子

WEKO 712470

en 羽鳥 晶子

Search repository
謝 琳

× 謝 琳

WEKO 712471

en 謝 琳

Search repository
脇坂 秀克

× 脇坂 秀克

WEKO 712472

en 脇坂 秀克

Search repository
栗原 雄祐

× 栗原 雄祐

WEKO 712473

en 栗原 雄祐

Search repository
大久保 崇之

× 大久保 崇之

WEKO 712474

en 大久保 崇之

Search repository
小川 政直

× 小川 政直

WEKO 712475

en 小川 政直

Search repository
念垣 信樹

× 念垣 信樹

WEKO 712476

en 念垣 信樹

Search repository
張 明栄

× 張 明栄

WEKO 712477

en 張 明栄

Search repository
抄録
内容記述タイプ Abstract
内容記述 Objectives: Growth hormone secretagogue receptor 1a (GHS-R1a) is a G protein-coupled receptor and expressed predominantly in the pituitary gland, at lower levels in the brain regions including hypothalamus that regulate feeding behavior and glucose sensing, and at even lower level in the pancreas. Therefore, GHSR1a is a promising drug target for complex neuroendocrine disorders that involve in both the central nervous system and the endocrine system. Recently, we developed PET probes for imaging of GHS-R1a ([18F]FEGRL1 and [11C]GRL2). These PET probes showed moderate uptake and low specific binding in the brain and pancreas. To improve uptake of radioactivity and specific binding in the brain and pancreas, we searched new candidate agents for a useful PET probe. Among the investigated compounds, (S)-(4-(1H-indole-6-carbonyl)-3-methylpiperazin-1-yl)(4’-methoxy-[1,1’-biphenyl]-4-yl)methanone (GRL3) has a high selective affinity for GHS-R1a (IC50 = 7.0 nmol/L)[1], and is possible for 11C labeling. Thus, we developed [11C]GRL3 as a new PET probe for imaging of GHS-R1a in the brain and pancreas.
Methods: [11C]GRL3 was synthesized by the methylation of its precursor (1.0 mg) with [11C]methyl iodide in the presence of 0.5 mol/L sodium hydroxide solution (5 μL) at 80ºC for 5 min. Biodistribution studies were conducted in mice.
Results: In the radiosynthesis, the decay-corrected radiochemical yield from 11CO2 was 43±8% (n = 10) at the end of radionuclide production, the molar radioactivity was 104±64 GBq/μmol (n = 15) at the end of synthesis, the radiochemical purity was >99%, and the synthesis time was approximately 30 min. In the biodistribution, radioactivity level of pancreas was highest (6.5 %ID/g) and that of brain was lowest (0.4 %ID/g) among all investigated tissues at 60 min after the injection. The radioactivity level in pancreas was gradually increased until 30 min after the injection, and maintained for 60 min after the injection. By pretreatment with YIL-781, which has high and selective affinity for GHS-R1a, the radioactivity level of pancreas at 30 min after the injection was significantly reduced to 55% of control, but that of brain was not changed.
Conclusions: [11C]GRL3 was successfully synthesized as an injection, and showed relatively high uptake and specific binding of the pancreas in mice. [11C]GRL3 may be a useful PET probe for imaging of GHS-R1a in the pancreas.
会議概要(会議名, 開催地, 会期, 主催者等)
内容記述タイプ Other
内容記述 22nd International symposium on radiopharmaceutical science (ISRS)
発表年月日
日付 2017-05-15
日付タイプ Issued
戻る
0
views
See details
Views

Versions

Ver.1 2023-05-15 19:41:00.996591
Show All versions

Share

Mendeley Twitter Facebook Print Addthis

Cite as

エクスポート

OAI-PMH
  • OAI-PMH JPCOAR
  • OAI-PMH DublinCore
  • OAI-PMH DDI
Other Formats
  • JSON
  • BIBTEX

Confirm


Powered by WEKO3


Powered by WEKO3