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Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents

Various radiometal complexes have been developed for tumor imaging, especially Ga-68 tracer. In the present study, the development of a radiogallium bis-thiosemicarbazone complex has been reported. [(67)Ga] acetylacetonate bis(thiosemicarbazone) complex ([(67)Ga] AATS) was prepared starting [(67)Ga]...

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Detalles Bibliográficos
Autores principales: Jalilian, Amir Reza, Yousefnia, Hassan, Shafaii, Kamaleddin, Novinrouz, Aytak, Rajamand, Amir Abbas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3832152/
https://www.ncbi.nlm.nih.gov/pubmed/24250475
Descripción
Sumario:Various radiometal complexes have been developed for tumor imaging, especially Ga-68 tracer. In the present study, the development of a radiogallium bis-thiosemicarbazone complex has been reported. [(67)Ga] acetylacetonate bis(thiosemicarbazone) complex ([(67)Ga] AATS) was prepared starting [(67)Ga]Gallium acetate and freshly prepared acetylacetonate bis (thiosemicarbazone) (AATS) in 30 min at 90°C. The partition co-efficient and the stability of the tracer were determined in final solution (25°C) and the presence of human serum (37°C) up to 24 h. The biodistribution of the labeled compound in wild-type and fibrosarcoma-bearing rodents were determined up to 72 h. The radiolabled Ga complex was prepared in high radiochemical purity (> 97%, HPLC) followed by initial biodistribution data with the significant tumor accumulation of the tracer in 2 h which is far higher than free Ga-67 cation while the compound wash-out is significantly faster. Above-mentioned pharmacokinetic properties suggest an interesting radiogallium complex while prepared by the PET Ga radioisotope, (68)Ga, in accordance with the physical half life, for use in fibrosarcoma tumors, and possibly other malignancies.