Synthesis, characterization and biodistribution of novel amine thiophene 99mTc labeled complex

Abstract

99mTc-labeled amine thiophene ligand might be a potential candidate for brain imaging. The purpose was to investigate the uptake of a radiolabeled drug in the brain. In this study, a tetradentate amine-thiophene-dione ligand was synthesized by the reaction of thiophene-2-carboxaldehyde with ethane-1,2-diamine and reducing with NaBH4. The ligand system was characterized by elemental analysis, FTIR and 1 H NMR. Radiolabeling of the complex with 99mTc was performed by reducing with stannous ions. The radiochemical purity of the radiolabeled drug was determined by paper chromatography (PC) and instant thin layer chromatography (ITLC). Bioevaluation of the 99mTc complex was studied in rabbits. The yield of the final product was 4.42 g (60%) and the characterization data confirmed the synthesis of the final product. The efficacy of radiolabeling was >98%. A significant uptake was observed in the brain which retained significantly upto 4h. The data indicate that the proposed system may be suitable for brain imaging in future clinical applications.