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oai:kanazawa-u.repo.nii.ac.jp:00015377 2024-06-27T01:25:29Z 2268:2269:2270

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 Ogawa, Kazuma 87 30347471 30347471 30347471 Takai, Kenichiro 27938 Kanbara, Hiroya 27939 Kiwada, Tatsuto 729 50414131 50414131 50414131 Kitamura, Youji 22945 10368483 10368483 Shiba, Kazuhiro 43 40143929 40143929 40143929 Odani, Akira 102 60143913 60143913 60143913 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 journal article Elsevier 2011-01-01 AM application/pdf Nuclear Medicine and Biology 5 38 631 636 AA10864894 0969-8051 https://kanazawa-u.repo.nii.ac.jp/record/15377/files/PH-PR-OGAWA-K-2011.pdf https://doi.org/10.24517/00015364 http://hdl.handle.net/2297/27077 https://kanazawa-u.repo.nii.ac.jp/records/15377 eng 10.1016/j.nucmedbio.2010.12.004