Synthesis and evaluation of 99mTc–2-[(3-carboxy-1-oxopropyl)amino]-2-deoxy-d-glucose as a potential tumor imaging agent |
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Institution: | 1. Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China;2. Department of Nuclear Medicine, Beijing Friendship Hospital of Capital Medical University, Beijing, China |
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Abstract: | The 2-(3-carboxy-1-oxopropyl)amino]-2-deoxy-d-glucose (CPADG) was synthesized and radiolabeled with 99mTcO4? to obtain the 99mTc–CPADG complex in high yield. It was stable over 6 h in saline at room temperature and in serum at 37 °C. The partition coefficient and electrophoresis results indicated that the complex was hydrophilic and cationic. In vitro cell studies showed there was an increase in the uptake of 99mTc–CPADG as a function of incubation time and 99mTc–CPADG was possibly transported via the glucose transporters. The biodistribution of 99mTc–CPADG in mice bearing S 180 tumor showed that the complex accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time and reached 1.91 and 5.05 at 4 h post-injection. Single photon emission computed tomography (SPECT) image studies showed there was an obvious accumulation in tumor sites, suggesting 99mTc–CPADG would be a promising candidate for tumor imaging. |
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Keywords: | Glucose Technetium-99m SPECT Tumor Imaging |
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