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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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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
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author Jalilian, Amir Reza
Yousefnia, Hassan
Shafaii, Kamaleddin
Novinrouz, Aytak
Rajamand, Amir Abbas
author_facet Jalilian, Amir Reza
Yousefnia, Hassan
Shafaii, Kamaleddin
Novinrouz, Aytak
Rajamand, Amir Abbas
author_sort Jalilian, Amir Reza
collection PubMed
description 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.
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spelling pubmed-38321522013-11-18 Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents Jalilian, Amir Reza Yousefnia, Hassan Shafaii, Kamaleddin Novinrouz, Aytak Rajamand, Amir Abbas Iran J Pharm Res Original Article 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. Shaheed Beheshti University of Medical Sciences 2012 /pmc/articles/PMC3832152/ /pubmed/24250475 Text en © 2012 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Jalilian, Amir Reza
Yousefnia, Hassan
Shafaii, Kamaleddin
Novinrouz, Aytak
Rajamand, Amir Abbas
Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents
title Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents
title_full Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents
title_fullStr Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents
title_full_unstemmed Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents
title_short Preparation and Biodistribution Studies of a Radiogallium-Acetylacetonate Bis (Thiosemicarbazone) Complex in Tumor-Bearing Rodents
title_sort preparation and biodistribution studies of a radiogallium-acetylacetonate bis (thiosemicarbazone) complex in tumor-bearing rodents
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3832152/
https://www.ncbi.nlm.nih.gov/pubmed/24250475
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