DO2A-based ligands for gallium-68 chelation: synthesis, radiochemistry and ex vivo cardiac uptake?
Dalton Transactions Pub Date: 2019-12-17 DOI: 10.1039/C9DT02354B
Abstract
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?D7.4 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.
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Journal Name：Dalton Transactions
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CAS no.: 89640-58-4
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