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論文
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梅崎, 実 ; 外山, 貴士 ; 杉本, 勝也 ; 山本, 和高 ; 石井, 靖
概要:
福井医科大学 第4内科<br />原著論文/症例報告
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佐藤, あかね ; 中島, 鉄夫 ; 外山, 貴士 ; 杉本, 勝也 ; 小鳥, 輝男
概要:
福井医科大学 放射線<br />原著論文/症例報告
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論文
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Ogawa, Kazuma ; Takai, Kenichiro ; Kanbara, Hiroya ; Kiwada, Tatsuto ; Kitamura, Youji ; Shiba, Kazuhiro ; Odani, Akira
概要:
金沢大学医薬保健研究域薬学系<br />Introduction: 68Ga is a radionuclide of great interest as a positron emitter for positron emission t
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omography (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.
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