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Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging

The optimization of the radiolabeling yield of carvedilol with iodine-131 was described. Dependence of the labeling yield of [(131)I]iodocarvedilol on the concentration of carvedilol, chloramine-T content, pH of the reaction mixture and reaction time was studied in details. Carvedilol was labeled wi...

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Autores principales: Motaleb, M. A., Attalah, K M, Shweeta, H A, Ibrahim, I. T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10018969/
https://www.ncbi.nlm.nih.gov/pubmed/36922888
http://dx.doi.org/10.1186/s13065-023-00935-0
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author Motaleb, M. A.
Attalah, K M
Shweeta, H A
Ibrahim, I. T.
author_facet Motaleb, M. A.
Attalah, K M
Shweeta, H A
Ibrahim, I. T.
author_sort Motaleb, M. A.
collection PubMed
description The optimization of the radiolabeling yield of carvedilol with iodine-131 was described. Dependence of the labeling yield of [(131)I]iodocarvedilol on the concentration of carvedilol, chloramine-T content, pH of the reaction mixture and reaction time was studied in details. Carvedilol was labeled with iodine-131 at pH 6 with a labeling yield of 92.6 ± 2.77% by using 100 µg carvedilol, 200 µg chloramin-T (CAT) and 30 min reaction time. The formed [(131)I]iodocarvedilol was nearly stable for a time up to one day. Biodistribution of [(131)I]iodocarvedilol was investigated in experimental animals. [(131/123)I]iodocarvedilol was located in the heart with a concentration of 19.6 ± 0.41% of the injected dose at 60 min post injection. It has a high heart uptake and heart to liver ratio, both of which are beneficial for high-quality SPECT (single-photon emission computerized tomography) myocardial imaging. [(131/123)I]iodocarvedilol solve most the drawbacks of the FDA (Food and Drug Administration) approved (99m)Tc-sestamibi.
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spelling pubmed-100189692023-03-17 Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging Motaleb, M. A. Attalah, K M Shweeta, H A Ibrahim, I. T. BMC Chem Research The optimization of the radiolabeling yield of carvedilol with iodine-131 was described. Dependence of the labeling yield of [(131)I]iodocarvedilol on the concentration of carvedilol, chloramine-T content, pH of the reaction mixture and reaction time was studied in details. Carvedilol was labeled with iodine-131 at pH 6 with a labeling yield of 92.6 ± 2.77% by using 100 µg carvedilol, 200 µg chloramin-T (CAT) and 30 min reaction time. The formed [(131)I]iodocarvedilol was nearly stable for a time up to one day. Biodistribution of [(131)I]iodocarvedilol was investigated in experimental animals. [(131/123)I]iodocarvedilol was located in the heart with a concentration of 19.6 ± 0.41% of the injected dose at 60 min post injection. It has a high heart uptake and heart to liver ratio, both of which are beneficial for high-quality SPECT (single-photon emission computerized tomography) myocardial imaging. [(131/123)I]iodocarvedilol solve most the drawbacks of the FDA (Food and Drug Administration) approved (99m)Tc-sestamibi. Springer International Publishing 2023-03-15 /pmc/articles/PMC10018969/ /pubmed/36922888 http://dx.doi.org/10.1186/s13065-023-00935-0 Text en © The Author(s) 2023 https://creativecommons.org/licenses/by/4.0/Open AccessThis article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) . The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/ (https://creativecommons.org/publicdomain/zero/1.0/) ) applies to the data made available in this article, unless otherwise stated in a credit line to the data.
spellingShingle Research
Motaleb, M. A.
Attalah, K M
Shweeta, H A
Ibrahim, I. T.
Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging
title Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging
title_full Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging
title_fullStr Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging
title_full_unstemmed Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging
title_short Synthesis and biological evaluation of [(131)I]iodocarvedilol as a potential radiopharmaceutical for heart imaging
title_sort synthesis and biological evaluation of [(131)i]iodocarvedilol as a potential radiopharmaceutical for heart imaging
topic Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10018969/
https://www.ncbi.nlm.nih.gov/pubmed/36922888
http://dx.doi.org/10.1186/s13065-023-00935-0
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