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DO2A-based ligands for gallium-68 chelation: Synthesis, radiochemistry and: Ex vivo cardiac uptake

Research output: Contribution to journalArticle

Adam J. Smith, Bradley E. Osborne, George P. Keeling, Philip J. Blower, Richard Southworth, Nicholas J. Long

Original languageEnglish
Pages (from-to)1097-1106
Number of pages10
JournalDalton Transactions
Volume49
Issue number4
DOIs
Published1 Jan 2020

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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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