Počet záznamů: 1
Radiolabelled Cyclic Bisarylmercury: High Chemical and in vivo Stability for Theranostics
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SYSNO ASEP 0543918 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Radiolabelled Cyclic Bisarylmercury: High Chemical and in vivo Stability for Theranostics Tvůrce(i) Gilpin, I. M. F. (DE)
Ullrich, M. (DE)
Wunsche, T. (DE)
Zarschle, K. (DE)
Lebeda, Ondřej (UJF-V) RID, ORCID, SAI
Pietzsch, J. (DE)
Pietzsch, H. -J. (DE)
Walther, M. (DE)Celkový počet autorů 8 Zdroj.dok. ChemMedChem. - : Wiley - ISSN 1860-7179
Roč. 16, č. 17 (2021), s. 2645-2649Poč.str. 6 s. Forma vydání Tištěná - P Jazyk dok. eng - angličtina Země vyd. DE - Německo Klíč. slova Bispidine ; Mercury ; Organomercury ; Radiopharmaceuticals ; Theranostics Vědní obor RIV FR - Farmakologie a lékárnická chemie Obor OECD Pharmacology and pharmacy Způsob publikování Open access Institucionální podpora UJF-V - RVO:61389005 UT WOS 000661839600001 EID SCOPUS 85107974096 DOI 10.1002/cmdc.202100131 Anotace We show the synthesis of an in vivo stable mercury compound with functionality suitable for radiopharmaceuticals. The designed cyclic bisarylmercury was based on the water tolerance of organomercurials, higher bond dissociation energy of Hg-Ph to Hg-S, and the experimental evidence that acyclic structures suffer significant cleavage of one of the Hg-R bonds. The bispidine motif was chosen for its in vivo stability, chemical accessibility, and functionalization properties. Radionuclide production results in (HgCl2)-Hg-197(m)(aq), so the desired mercury compound was formed via a water-tolerant organotin transmetallation. The Hg-bispidine compound showed high chemical stability in tests with an excess of sulfur-containing competitors and high in vivo stability, without any observable protein interaction by human serum assay, and good organ clearance demonstrated by biodistribution and SPECT studies in rats. In particular, no retention in the kidneys was observed, typical of unstable mercury compounds. The Hg-nat analogue allowed full characterization by NMR and HRMS. Pracoviště Ústav jaderné fyziky Kontakt Markéta Sommerová, sommerova@ujf.cas.cz, Tel.: 266 173 228 Rok sběru 2022 Elektronická adresa https://doi.org/10.1002/cmdc.202100131
Počet záznamů: 1