Synthesis and preliminary evaluation of mono-[I-123]iodohypericin monocarboxylic acid as a necrosis avid imaging agent

University of Leuven, Louvain, Flemish, Belgium
Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.33). 07/2007; 17(14):4001-5. DOI: 10.1016/j.bmcl.2007.04.083
Source: PubMed

ABSTRACT Hypericin monocarboxylic acid was synthesized in an overall yield of 25% in four steps and radiolabelled with iodine-123 in good yield (>75%). The resulting mono-[(123)I]iodohypericin monocarboxylic acid was evaluated in normal mice and in rats with ethanol induced liver necrosis. In this model, tracer concentration in necrotic liver tissue was 14 times higher than in the viable liver tissue as quantified by autoradiography at 24h post injection. The results indicate the feasibility of visualization of necrotic tissue with the novel tracer.

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