Preparation and preclinical pharmacological study on a novel bone imaging agent ^99mTc-EMIDP

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• 作者：Jianguo Lin ; Shineng Luo ; Chuanqing Chen ; Ling Qiu ; Yan Wang ; Wen Cheng ; Wanzhong Ye ; Yongmei Xia
• 关键词：Diphosphonic acid ; ^99mTc-EMIDP ; Biodistribution ; Bone imaging agent
• 刊名：Applied Radiation and Isotopes
• 出版年：2010
• 出版时间：September 2010
• 年：2010
• 卷：68
• 期：9
• 页码：1616-1622
• 全文大小：426 K

文摘

A novel zoledronic acid (ZL) derivative, 1-hydroxy-2-(2-ethyl-4-methyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (EMIDP), was prepared and labeled with ^99mTc successfully in a high labeling yield and good stability in vitro. The preclinical pharmacological properties of ^99mTc-EMIDP were investigated and compared with ^99mTc-MDP and ^99mTc-ZL. The studies of biodistribution in mice and SPECT bone imaging of the rabbit suggest that ^99mTc-EMIDP has highly selective uptake in the skeletal system and rapid clearance in the soft tissues. The present findings indicate that ^99mTc-EMIDP holds great potential for bone scintigraphy.