Radiolabeled l-Lysine for Tumor Imaging

作者: Alper O. Karacalioglu , David J. Yang , Ali Azhdarinia , Richard Mendez , Changsok Oh

DOI: 10.1016/J.ACRA.2006.03.022

关键词:

摘要: Rationale and Objectives The aims of this study were to label the versatile amino acid l -lysine with 99m Tc using 2,3-dimercapto-succinic (DMSA) as a chelator, assess its tumor imaging feasibility under in vivo vitro conditions, finally determine subcellular biodistribution radiopharmaceutical. Materials Methods DMSA- was chemically synthesized labeled sodium pertechnetate. Nuclear magnetic resonance (NMR) mass spectral analysis conducted. Radiochemical purity determined by thin-layer chromatography (TLC) paper chromatography. Cellular uptake, competition localization studies performed rat breast cancer cells (13762). In planar on female Fischer 344 rats. Medical Internal Radiation Dose (MIRD) dosimetry estimates calculated. Results (determined radio-TLC high-performance liquid chromatography) these compounds >95%. Tc-DMSA- showed good uptake cell culture assays reduced studies. accumulates nucleus much cytoplasm it also shown that accumulation increases function time. There an increase tumor-to-blood tumor-to-muscle count density ratios. Tumor/background ratios 5.75 at 1 hour 6.87 2 hours. tissue distribution revealed radiation blood-forming organs within dose limits. Conclusion kits can be easily efficiently, high radiochemical cost-effectiveness. cellular scintigraphic demonstrated pharmacokinetic for imaging.

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