Synthesis and 99m Tc Labeling Iminodiacetic Acid Analogues：A Hepatobiliary Imaging Agent in Nuclear Medicine

• Main Authors: Chao-Yao Peng, 彭肇堯
• Other Authors: Yu-ling Lu
• Format: Others
• Language: zh-TW
• Published: 2012
• Online Access: http://ndltd.ncl.edu.tw/handle/4df656

碩士 === 嘉南藥理科技大學 === 藥物科技研究所 === 100 === In the present study, we design and synthesized of 99mTc labeling IDA compounds 7a and 7b. In vitro cytotoxicity assays of these compounds, data showed that 7a and 7b were nontoxic for various cancer cell lines. Therefore, we did not warred about hepatotoxicity as a hepatobiliary imaging agent. For a nuclear medicine imaging comparison, three different 99mTc-IDA derivatives, 99mTc-Hepatolite®, 99mTc-7a (8a) and 99mTc-7b (8b), were prepared and evaluated for their in vivo biodistribution through animal models. Serial static image scans of rabbits injected with 99mTc-7a (8a) revealed that higher radioactivity concentrations of the liver compared to the heart or kidneys. This result clearly showed that 7a showed selective distribution to the hepatobiliary system. In contrast, the distribution ratio of 99mTc-7b (8b) was low level to the liver, hence 7b is not suitable as a hepatobiliary imaging agent. Although, the liver selective of 99mTc-7a (8a) has not better than commercial source (99mTc-Hepatolite®), the radioactivity of the live also show six fold difference than the heart or kidneys. In this study, we developed a novel aimnobiphenyl as prototypical lead compound for hepatobiliary system. We further modify 7a via electrophilic substitution protons of biphenyl ring, expect for selective distribution to the hepatobiliary system, the further may be provide a perfect candidate for hepatobiliary imaging.