DO2A-based ligands for gallium-68 chelation: synthesis, radiochemistry and cardiac uptake
Radiolabelled lipophilic cations could potentially be used to non-invasively image mitochondrial dysfunction in cardiovascular disease, building on their current role as perfusion imaging agents. We have synthesised and radiolabelled two series of DO2A-based radiotracers, with bistriarylphosphonium-...
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Published in | Dalton transactions : an international journal of inorganic chemistry Vol. 49; no. 4; pp. 197 - 116 |
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Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
28.01.2020
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Online Access | Get full text |
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Summary: | Radiolabelled lipophilic cations could potentially be used to non-invasively image mitochondrial dysfunction in cardiovascular disease, building on their current role as perfusion imaging agents. We have synthesised and radiolabelled two series of DO2A-based radiotracers, with bistriarylphosphonium- and bisaryl-functionalisation respectively, with gallium-68 to form lipophilic cations. Both sets of tracers radiolabel with over 90% RCP, although the tracers form kinetic/thermodynamic pairs of species upon gallium chelation that can be visualised and separated by radioHPLC. Log
D
7.4
values above −0.3 are observed for the most lipophilic examples of each series of radiotracers. Both tracers show significant preferential uptake in healthy cardiac tissue over cardiac tissue depolarised by CCCP.
New DO2A-based lipophilic and cationic chelators for gallium-68 have been synthesised for cardiac PET imaging. These radiotracers show preferential uptake in healthy cardiac tissue over cardiac tissue depolarised by CCCP. |
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Bibliography: | 10.1039/c9dt02354b Electronic supplementary information (ESI) available. See DOI |
ISSN: | 1477-9226 1477-9234 |
DOI: | 10.1039/c9dt02354b |