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Preparation and in vivo biological investigation of 99m Tc‐HEIDP as a novel radioligand for bone scanning
Author(s) -
Qiu Ling,
Xue Li,
Chen Yongshi,
Lin Jianguo,
Nan Beibei,
Cheng Wen,
Luo Shineng
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2941
Subject(s) - chemistry , radioligand , biodistribution , in vivo , radiochemistry , yield (engineering) , bone imaging , half life , kinetics , nuclear chemistry , tracer , nuclear medicine , pharmacokinetics , in vitro , biochemistry , pharmacology , medicine , materials science , physics , microbiology and biotechnology , quantum mechanics , nuclear physics , metallurgy , biology
A novel diphosphonic acid, 1‐hydroxy‐2‐(1‐ethyl‐imidazol‐2‐yl) ethane‐1,1‐diphosphonic acid (HEIDP), was prepared and labeled with 99m Tc in a high labeling yield under optimized labeling conditions. The biodistribution in mice shows that 99m Tc‐HEIDP has high specificity and efficacy in bone and joint uptake with 5.73 and 9.93%ID/g at 5 min, which increases continuously to a maximum of 7.62 and 18.0%ID/g at 30 min, respectively. Kinetics of blood clearance showed that distribution half‐life ( T 1/2α ) and elimination half‐life ( T 1/2β ) of 99m Tc‐HEIDP were 9.91 and 81.1 min, respectively. The total clearance rate was 1.94%ID/g•min ‐1 . A plain and clear bone image was obtained at 1 h by using single photon emission computed tomography. All results indicate that 99m Tc‐HEIDP holds potential as a superior tracer agent for bone scanning. Copyright © 2012 John Wiley & Sons, Ltd.