title: Synthesis, characterization and biodistribution of novel amine thiophene ⁹⁹mTc labeled complex.
abstract: (99m)Tc-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 NaBH(4). The ligand system was characterized by elemental analysis, FTIR and 1H NMR. Radiolabeling of the complex with (99m)Tc 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 (99m)Tc 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.
authors.affiliation: Radiopharmacy Division, Institute of Nuclear Medicine & Oncology (INMOL), New Campus Road, P. O. Box 10068, Lahore, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Javed
authors.forename: Irfanullah
authors.initials: I
authors.lastname: Khan
authors.forename: Saima
authors.initials: S
authors.lastname: Mobeen
authors.forename: Ume-Kalsoom
authors.initials: UK
authors.lastname: Dar
authors.forename: Syed Waqar
authors.initials: SW
authors.lastname: Hyder
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D001921:Brain / Q000378:metabolism*; D006801:Humans; D007553:Isotope Labeling; D008024:Ligands; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011485:Protein Binding; D011817:Rabbits; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D000588:Amines; D008024:Ligands; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D013876:Thiophenes