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Radiolabelled Cyclic Bisarylmercury: High Chemical and in vivo Stability for Theranostics
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SYSNO ASEP 0543918 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Radiolabelled Cyclic Bisarylmercury: High Chemical and in vivo Stability for Theranostics Author(s) 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)Number of authors 8 Source Title ChemMedChem. - : Wiley - ISSN 1860-7179
Roč. 16, č. 17 (2021), s. 2645-2649Number of pages 6 s. Publication form Print - P Language eng - English Country DE - Germany Keywords Bispidine ; Mercury ; Organomercury ; Radiopharmaceuticals ; Theranostics Subject RIV FR - Pharmacology ; Medidal Chemistry OECD category Pharmacology and pharmacy Method of publishing Open access Institutional support UJF-V - RVO:61389005 UT WOS 000661839600001 EID SCOPUS 85107974096 DOI 10.1002/cmdc.202100131 Annotation 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. Workplace Nuclear Physics Institute Contact Markéta Sommerová, sommerova@ujf.cas.cz, Tel.: 266 173 228 Year of Publishing 2022 Electronic address https://doi.org/10.1002/cmdc.202100131
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