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Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent
https://doi.org/10.24517/00015364
https://doi.org/10.24517/0001536497b05a65-fed4-432b-90c0-026315031672
名前 / ファイル | ライセンス | アクション |
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PH-PR-OGAWA-K-2011.pdf (93.8 kB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2017-10-04 | |||||
タイトル | ||||||
タイトル | Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent | |||||
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 | |||||
ID登録 | ||||||
ID登録 | 10.24517/00015364 | |||||
ID登録タイプ | JaLC | |||||
著者 |
Ogawa, Kazuma
× Ogawa, Kazuma× Takai, Kenichiro× Kanbara, Hiroya× Kiwada, Tatsuto× Kitamura, Youji× Shiba, Kazuhiro× Odani, Akira |
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著者別表示 |
小川, 数馬
× 小川, 数馬× 黄檗, 達人× 北村, 暘二× 柴, 和弘× 小谷, 明 |
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提供者所属 | ||||||
内容記述タイプ | Other | |||||
内容記述 | 金沢大学新学術創成研究機構 / 金沢大学医薬保健研究域薬学系 | |||||
書誌情報 |
Nuclear Medicine and Biology 巻 38, 号 5, p. 631-636, 発行日 2011-01-01 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0969-8051 | |||||
NCID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA10864894 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.nucmedbio.2010.12.004 | |||||
出版者 | ||||||
出版者 | Elsevier | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Introduction: 68Ga is a radionuclide of great interest as a positron emitter for positron emission tomography (PET). To develop a new bone-imaging agent with radiogallium, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) was chosen as a chelating site and Ga-DOTA complex-conjugated bisphosphonate, which has a high affinity for bone, was prepared and evaluated. Although we are interested in developing 68Ga-labeled bone imaging agents for PET, in these initial studies 67Ga was used because of its longer half-life. Methods: DOTA-conjugated bisphosphonate (DOTA-Bn-SCN-HBP) was synthesized by conjugation of 2-(4-isothiocyanatebenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid to 4-amino-1-hydroxybutylidene-1,1-bisphosphonate (alendronate). 67Ga-DOTA-Bn-SCN-HBP was prepared by coordination with 67Ga, and its in vitro and in vivo evaluations were performed. Results: 67Ga-DOTA-Bn-SCN-HBP was prepared with a radiochemical purity of over 95% without purification. 67Ga-DOTA-Bn-SCN-HBP had great affinity for hydroxyapatite in binding assay. In biodistribution experiments, 67Ga-DOTA-Bn-SCN-HBP accumulated in bone rapidly but was hardly observed in tissues other than bone. Pretreatment of an excess amount of alendronate inhibited the bone accumulation of 67Ga-DOTA-Bn-SCN-HBP. Conclusions: 67Ga-DOTA-Bn-SCN-HBP showed ideal biodistribution characteristics as a bone-imaging agent. These findings should provide useful information on the drug design of bone imaging agents for PET with 68Ga. © 2010 Elsevier Inc. All rights reserved. | |||||
著者版フラグ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa |