Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf
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99mTc-labelled RGD-Peptide using the "4+1" mixed-ligand approachGiglio, J.; León, E.; Rey, A.; Künstler, J.-U.; Gniazdowska, E.; Pietzsch, H.-J.
This paper presents the 99mTc-labelling and evaluation of two isocyanide (4-isocyanomethylbenzoic acid = L1, 4-isocyanobutanoic acid= L2) derivatives of the peptide c(RGDyK) using the "4+1" mixed-ligand chelate system. Starting from the precursor 99mTc-EDTA labelling was achieved by reaction of the isocyanide-bearing peptide and the tetradentate ligand containing three non-coordinating carboxyl groups (NS3(COOH)3) resulting in 99mTc(NS3(COOH)3)(L1-c(RGDyK)), 1 and 99mTc(NS3(COOH)3)(L2-c(RGDyK)), 2. A radiochemical purity (RP) of 60% was obtained for both peptides and HPLC purification resulted in RP>95% and stability was >90% after 24h. Plasma protein binding was 27% for 1 and 15% for 2. Both complexes showed preferential renal excretion. Uptake in induced B16F1 murine melanoma was moderate for both compounds but higher tumour/muscle ratios were achieved for 1 at all time points.
Keywords: Tc "4+1" mixed-ligand complexes, 99mTc labelled peptides, RGD peptides
7th International Symposium on Technetium in Chemistry and Nuclear Medicine, 06.-09.09.2006, Bressanone, Italy
Contribution to external collection
U. Mazzi: Technetium, Rhenium and Other Metals in Chemistry and Nuclear Medicine, Padova: SGE Editoriali, 2006, 88-89884-04-5, 331-332