Synthesis and bio-evaluation of a new fatty acid derivative for myocardial imaging

Add time:09/07/2019    Source:sciencedirect.com

Development of a 99mTc-fatty acid analogue is of interest, as 99mTc is logistically advantageous over the cyclotron-produced 11C and 123I. Synthesis of a 16 carbon fatty acid derivative and its radiolabeling with the novel [99mTcN(PNP)]2+ core is described here. Hexadecanedioic acid was conjugated to cysteine in an overall yield of 55%. This ligand could be labeled with 99mTc via the [99mTcN(PNP)]2+ core, in 80% yield, as a mixture of two isomers (syn and anti). The major isomer isolated by HPLC was used for bioevaluation studies in swiss mice and compared with radioiodinated iodophenyl pentadecanoic acid (IPPA), an established agent for myocardial metabolic imaging. 99mTc-labeled complex cleared faster from the non-target organs, namely, liver, lungs, and blood compared to that of [125I]-IPPA. However, the complex exhibited lower uptake and faster washout from the myocardium as compared to [125I]-IPPA.

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