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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]...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Shaheed Beheshti University of Medical Sciences
2012
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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. |
format | Online Article Text |
id | pubmed-3832152 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | Shaheed Beheshti University of Medical Sciences |
record_format | MEDLINE/PubMed |
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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