Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

フォーマット:

論文

責任表示:

Ogawa, Kazuma ; Takai, Kenichiro　 ; Kanbara, Hiroya　 ; Kiwada, Tatsuto ; Kitamura, Youji ; Shiba, Kazuhiro ; Odani, Akira

言語:

英語

出版情報:

Elsevier, 2011-01-01

著者名:

Ogawa, Kazuma

Takai, Kenichiro

Kanbara, Hiroya

Kiwada, Tatsuto

Kitamura, Youji

Shiba, Kazuhiro

Odani, Akira

続きを見る

掲載情報:

Nuclear Medicine and Biology

ISSN:

0969-8051      

巻:

xx

通号:

xx

開始ページ:

xxxx

終了ページ:

xxxx

バージョン:

author

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 tomography (PET). To develop a new bone-imaging agent with radiogallium, 1,4,7,10-tetraazacyclododecane-1,4,7,10-te … traacetic 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. 続きを見る

URL:

http://hdl.handle.net/2297/27077