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Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent 小川, 数馬 黄檗, 達人 北村, 暘二 柴, 和弘 小谷, 明 30347471 Ogawa, Kazuma Takai, Kenichiro Kanbara, Hiroya 50414131 Kiwada, Tatsuto Kitamura, Youji 40143929 Shiba, Kazuhiro 60143913 Odani, Akira 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. 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 Elsevier 2011-01-01 2017-10-04 eng journal article AM https://doi.org/10.24517/00015364 http://hdl.handle.net/2297/27077 https://kanazawa-u.repo.nii.ac.jp/records/15377 10.24517/00015364 10.1016/j.nucmedbio.2010.12.004 AA10864894 0969-8051 Nuclear Medicine and Biology 38 5 631 636 https://kanazawa-u.repo.nii.ac.jp/record/15377/files/PH-PR-OGAWA-K-2011.pdf application/pdf 93.8 kB 2017-10-04