Evaluation of chelating agents based on pyridine-azacrown compounds H4PATA, PATAM, and H4PATPA for 68Ga and 177Lu

Shchukina, A.A.; Zubenko, A.D.; Tarasenko, O.V.; Larenkov, A.A.; Bubenshchikov, V.B.; Chernikova, E.Y.; Fedorov, Y.V.; Fedorova, O.A.

Авторы: Shchukina Anna A., Zubenko Anastasia D., Tarasenko Oksana V., Larenkov Anton A., Bubenshchikov Viktor B., Chernikova Ekaterina Y., Fedorov Yury V., Fedorova Olga A.
Журнал: Nuclear Medicine and Biology
Том: 140
Год издания: 2025
Издательство: Elsevier BV
Местоположение издательства: Netherlands
Номер статьи: 108972
DOI: 10.1016/j.nucmedbio.2024.108972
Аннотация: In this article, we present the synthesis and characterization of three macrocyclic chelators, H4PATA, PATAM, and H4PATPA, based on a pyridine-azacrown compound. Their complexation with 68Ga and 177Lu has been thoroughly investigated using MALDI TOF MS, 1H NMR spectroscopy, radiolabeling studies, and experiments in vitro with fetal bovine serum and a 1000-fold molar excess of H4EDTA. Our studies have shown that the chelators H4PATA and H4PATPA form complexes at room temperature with both radionuclides (RCY > 80 % and > 90 % for complexes with H4PATA and H4PATPA after 30 min, respectively). The chelator PATAM requires high temperature (95 °C) for complexation. In vitro stability assays in fetal bovine serum as well as H4EDTA-challenge revealed that transchelation occurs for all complexes with 68Ga. However, complexes of the ligands H4PATA and PATAM with 177Lu were found stable. Thus, taking into account the radiolabeling at room temperature and in vitro stability of the complex [177Lu]Lu·PATA, our investigations revealed the chelator H4PATA is a candidate for radiopharmaceutical use with 177Lu.
Добавил в систему: Щукина Анна Алексеевна

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Evaluation of chelating agents based on pyridine-azacrown compounds H4PATA, PATAM, and H4PATPA for 68Ga and 177Luстатья

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