Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents
A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP)...
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Online Access: | http://www.mdpi.com/1420-3049/16/8/6165/ |
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doaj-fa70cc965e3a4c888907792e217c70dd2020-11-24T23:14:47ZengMDPI AGMolecules1420-30492011-07-011686165617810.3390/molecules16086165Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging AgentsShineng LuoLi XueJing PanLing QiuWen ChengJianguo LinA series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with 99mTc in high labeling yields. The in vitro stability and in vivo biodistribution of 99mTc-MIPrDP, 99mTc-MIBDP and 99mTc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer 99mTc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that 99mTc-MIPrDP holds great potential for use in bone imaging.http://www.mdpi.com/1420-3049/16/8/6165/zoledronic acid derivative99mTc-labelled diphosphonatesin vitro stabilitybiodistributionbone imaging agent |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Shineng Luo Li Xue Jing Pan Ling Qiu Wen Cheng Jianguo Lin |
spellingShingle |
Shineng Luo Li Xue Jing Pan Ling Qiu Wen Cheng Jianguo Lin Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents Molecules zoledronic acid derivative 99mTc-labelled diphosphonates in vitro stability biodistribution bone imaging agent |
author_facet |
Shineng Luo Li Xue Jing Pan Ling Qiu Wen Cheng Jianguo Lin |
author_sort |
Shineng Luo |
title |
Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents |
title_short |
Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents |
title_full |
Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents |
title_fullStr |
Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents |
title_full_unstemmed |
Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents |
title_sort |
synthesis and biological evaluation of novel 99mtc-labelled bisphosphonates as superior bone imaging agents |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2011-07-01 |
description |
A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with 99mTc in high labeling yields. The in vitro stability and in vivo biodistribution of 99mTc-MIPrDP, 99mTc-MIBDP and 99mTc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer 99mTc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that 99mTc-MIPrDP holds great potential for use in bone imaging. |
topic |
zoledronic acid derivative 99mTc-labelled diphosphonates in vitro stability biodistribution bone imaging agent |
url |
http://www.mdpi.com/1420-3049/16/8/6165/ |
work_keys_str_mv |
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