2,5-Diamino-5,5-diphosphonovaleric Acid as a Ligand for an Osteotropic 188Re Radiopharmaceutical

被引：0
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作者：
G. S. Tsebrikova
V. V. Ragulin
V. E. Baulin
K. E. German
A. O. Malysheva
O. E. Klement’eva
G. E. Kodina
A. A. Larenkov
E. A. Lyamtseva
N. A. Taratonenkova
M. V. Zhukova
A. Yu. Tsivadze
机构：
[1] Russian Academy of Sciences,A.N. Frumkin Institute of Physical Chemistry and Electrochemistry
[2] Russian Academy of Sciences,Institute of Physiologically Active Compounds
[3] Federal Medical Biological Agency of Russia,Burnazyan Federal Medical Biophysical Center
来源：
Russian Journal of General Chemistry | 2018年 / 88卷
关键词：
osteotropic radiopharmaceuticals; rhenium-188; 2,5-diamino-5,5-diphosphonovaleric acid; biological distribution;
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摘要：
A modified method for the preparation of 2,5-diamino-5,5-diphosphonovaleric acid (DADP5) has been developed in the search for new synthetically available organic ligands to produce 188Re radiopharmaceuticals with an increased accumulation in the bone tissue. Interaction of the obtained acid with 188Re was studied by radio-TLC. An optimal system for separating unbound 188Re and labeled complex in a yield of at least 95% was found. The biological distribution of 188Re-DADP5 was studied based on direct radiometric data. The osteotropicity of 188Re-DADP5 and its increased accumulation in bone fracture sites, which represent oncological pathology models, was detected at a level comparable to known radiopharmaceuticals.
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页码：1780 / 1785
页数：5
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