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J Cell Biochem ; 120(9): 14510-14517, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-30994957

RESUMO

Diethylenetriamine penta-acetic acid (DTPA), when complexed with a gamma (γ)-emitter radioisotope like 99m Tc, is used for renal function diagnosis and many other diagnostic applications. The main aim of this study was to develop a novel and versatile single-step methodology for the synthesis of a new 177 Lu-labeled radiopharmaceutical with high radiochemical yield, which can be used for diagnostic purposes and therapeutic purposes also. The single and well-defined 177 Lu-DTPA complex was radiochemically characterized by paper chromatography, thin-layer chromatography, high-performance liquid chromatography, and electrophoresis techniques. Dependence of the labeling yield of 177 Lu-DTPA complex on different factors was studied in detail. Biological evaluation was also performed in a normal rabbit by developing images under a γ camera at various time intervals. More than 99% labeling yield was obtained by reacting DTPA with 177 Lu at specific conditions (pH 7.0, 15 minutes reaction time at 100 °C). 177 Lu-DTPA complex showed high stability both at room temperature and in vitro. Biodistribution studies in normal mice indicated the fractional renal uptake of intravenously administered 177 Lu-DTPA complex, which reached in the kidneys within 2-3 minutes. Scintigraphy showed rapid clearance from the body. Based on these results, we propose that 177 Lu-DTPA complex might be used as an ideal candidate for functional evaluation of kidneys and the urinary tract, especially when needed to be transported to long-range consumer sites, because of its suitable half-life.


Assuntos
Lutécio/química , Ácido Pentético/farmacocinética , Radioisótopos/química , Compostos Radiofarmacêuticos/farmacocinética , Animais , Estabilidade de Medicamentos , Humanos , Masculino , Camundongos , Ácido Pentético/administração & dosagem , Ácido Pentético/síntese química , Ácido Pentético/química , Coelhos , Compostos Radiofarmacêuticos/administração & dosagem , Compostos Radiofarmacêuticos/síntese química , Compostos Radiofarmacêuticos/química , Distribuição Tecidual
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