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Issue 4, 2020
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DO2A-based ligands for gallium-68 chelation: synthesis, radiochemistry and ex vivo cardiac uptake

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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.

Graphical abstract: DO2A-based ligands for gallium-68 chelation: synthesis, radiochemistry and ex vivo cardiac uptake

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Supplementary files

Article information


Submitted
04 Jun 2019
Accepted
17 Dec 2019
First published
17 Dec 2019

Dalton Trans., 2020,49, 1097-1106
Article type
Paper

DO2A-based ligands for gallium-68 chelation: synthesis, radiochemistry and ex vivo cardiac uptake

A. J. Smith, B. E. Osborne, G. P. Keeling, P. J. Blower, R. Southworth and N. J. Long, Dalton Trans., 2020, 49, 1097
DOI: 10.1039/C9DT02354B

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