| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2017-10-04 |
| タイトル |
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タイトル |
Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent |
| 言語 |
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言語 |
eng |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| ID登録 |
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ID登録 |
10.24517/00015364 |
|
ID登録タイプ |
JaLC |
| 著者 |
Ogawa, Kazuma
Takai, Kenichiro
Kanbara, Hiroya
Kiwada, Tatsuto
Kitamura, Youji
Shiba, Kazuhiro
Odani, Akira
|
| 著者別表示 |
小川, 数馬
黄檗, 達人
北村, 暘二
柴, 和弘
小谷, 明
|
| 提供者所属 |
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|
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 |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
0969-8051 |
| NCID |
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収録物識別子タイプ |
NCID |
|
収録物識別子 |
AA10864894 |
| DOI |
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関連タイプ |
isVersionOf |
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|
識別子タイプ |
DOI |
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関連識別子 |
10.1016/j.nucmedbio.2010.12.004 |
| 出版者 |
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出版者 |
Elsevier |
| 抄録 |
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内容記述タイプ |
Abstract |
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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 |
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出版タイプ |
AM |
|
出版タイプResource |
http://purl.org/coar/version/c_ab4af688f83e57aa |
PH-PR-OGAWA-K-2011.pdf (93.8 kB)
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