Synthesis and biodistribution of a novel 99m Tc nitrido radiopharmaceutical with proline dithiocarbamate as a potential
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Synthesis and biodistribution of a novel 99mTc nitrido radiopharmaceutical with proline dithiocarbamate as a potential tumor imaging agent Miao Liu • Xiao Lin • Xiaoqing Song • Yang Cui • Peiwen Li • Xuebin Wang • Junbo Zhang
Received: 15 March 2013 Ó Akade´miai Kiado´, Budapest, Hungary 2013
Abstract In the present study, proline dithiocarbamate (PRODTC) ligand was radiolabeled with the [99mTc:N]2? core successfully to obtain the 99mTcN-PRODTC complex with high radiochemical purity. No decomposition of the complex at room temperature was observed over a period of 6 h. Its partition coefficient indicated that it was a hydrophilic complex. The electrophoresis results showed that the complex was negative. The biodistribution of 99m TcN-PRODTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with a certain uptake. The tumor/blood and tumor/muscle ratios reached 2.19 and 4.54 at 2 h post-injection, suggesting it would be a promising candidate for tumor imaging. Keywords Tumor imaging L-proline Dithiocarbamate [99mTcN]2? core
Introduction [18F]fluorodeoxyglucose [18F]FDG has been the most widely used radiotracer for tumor imaging. However, [18F]FDG can not distinguish tumor from inflammatory tissue or normal brain tissues. Amino acids play an important role in the growth of tumor cells, providing a good opportunity for their use in tumor imaging. The tumor imaging by using radiolabeled amino acids is less influ-
M. Liu X. Lin X. Song Y. Cui P. Li X. Wang J. Zhang (&) Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, People’s Republic of China e-mail: [email protected]
enced by inflammatory processes, suggesting they can overcome the limitation displayed by [18F]FDG [1]. Currently, many amino acids derivatives radiolabeled with positron emitters such as [11C]methionine ([11C]MET) [2, 3], L-3-[18F]fluoro-a-methyl-L-tyrosine ([18F]FMT) [4, 5], O-(2-[18F]-fluoroethyl)-L-tyrosine ([18F]FET) [6–8] and Cis-4-[18F]fluoro-L-proline(Cis-[18F]FPro) [9] have been developed for positron emission tomography (PET). However, a cyclotron is essential to produce these radionuclides, thus restricting their wide use in clinical practice. By comparison, 99mTc has been the isotope of choice for development of novel radiopharmaceuticals owing to its short half-life, optimal c-energy, inexpensive cost and diverse coordination chemistry. Therefore, achieving 99mTc labeled amino acids derivatives as single photon emission computed tomography (SPECT) probes is considered to be of great interest. Recently, several 99mTc labeled amino acids derivatives as tumor imaging agents have been reported [10–12]. Among them, 99mTc-diethylenetriaminepentaacetic acid-bis(methionine) (99mTc-DTPA-bis(Met)) shows the most promising character to be a tumor imaging agent. However, its chemical structure is poorly defined due to its complicated coordination structure. The preparation of novel 99mTc labeled amino acids derivatives is still
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