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Chelators tailored for preparation of 68Ga-labeled mono-, di- and trimeric bioconjugates

Publication at Faculty of Science |
2013

Abstract

Triazacyclononane triphosphinic acid derivatives TRAP [1-3] and NOPO [4], as well as their bioconjugates TRAP(RGD)3, NOPO-NOC and NOPO-RGD, show excellent (68)Ga-labeling properties [5] and promising in vivo biodistribution and pharmacokinetics. To cover the demands of current trends in tracer development, we preprared a series of phosphinate chelators with high selectivity for (68)Ga and tailored properties for different applications.

We present chelators for preparation of monoconjugates, dimeric and heterodimeric tracers, as well as chelators suitable for modifying the lipophilicity of 68Ga-radiopharmaceuticals.

Keywords