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Citation: CHENG Wen, LIN Jianguo, QIU Ling, YE Wanzhong, LUO Shineng. Preparation and in vivo Bone Imaging Properties of ^99mTc(Ⅳ)-Labeled Diphosphonic Acid Complex[J]. Chinese Journal of Applied Chemistry, ;2013, 30(5): 542-548. doi: 10.3724/SP.J.1095.2013.20300 shu

Preparation and in vivo Bone Imaging Properties of ^99mTc(Ⅳ)-Labeled Diphosphonic Acid Complex

Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China

Received Date: 6 July 2012
Revised Date: 31 October 2012

A zoledronic acid derivative,1-hydroxy-5-(2-ethyl-1H-imidazol-1-yl)pentane-1,1-diphosphonic acid(EIPeDP),was synthesized using 2-ethylimidazole,5-bromo valeric acid ethyl ester and PCl₃ as the starting material and further labeled with ^99mTc. The influence of the amount of EIPeDP and the pH value of the reaction system on the labeling yield of ^99mTc-EIPeDP has been studied. Satisfactory radiolabelling yield(RLY) and the radiochemical purity(RCP) (over 97%) were obtained when the pH was 5~6 and the amount of EIPeDP,SnCl₂·2H₂O and Na ^99mTcO₄ were 5 mg,100 μg and 92.5 MBq,respectively. The radiolabeled complex was very stable in vitro. In vivo SPECT bone imaging of rabbit showed that a clearer image can be obtained from ^99mTc-EIPeDP at 1 h post injection,which is superior to ^99mTc-ZL and ^99mTc-MDP. These results showed that ^99mTc-EIPeDP is a potential bone imaging agent with advantages of simple preparation,good stability and superior bone imaging characteristics.
- zoledronic acid derivative,
- ^99mTc radiolabeling,
- quality control,
- stability,
- bone imaging
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Preparation and in vivo Bone Imaging Properties of 99mTc(Ⅳ)-Labeled Diphosphonic Acid Complex

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通讯作者: 陈斌, bchen63@163.com

Preparation and in vivo Bone Imaging Properties of ^99mTc(Ⅳ)-Labeled Diphosphonic Acid Complex