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Radiolabelling of multimeric neurotensin(8-13) analogues with the short-lived positron emitter fluorine-18

Hultsch, C.; Berndt, M.; Bergmann, R.; Wüst, F.
Neurotensin receptors are expressed with high incidence in several human tumour entities. Thus, radiolabelled neurotensin derivatives might be used for tumour targeting. However, its application is limited by insufficient metabolic stability. Metabolic stability might be improved by the synthesis of multivalent peptides.
Three methods for 18F-labelling of dimeric and tetrameric
neurotensin(8-13) derivatives were evaluated with respect to the labelling yield and the required peptide amounts. Labelling using N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) gave low radiochemical yield for the dimeric peptides. Coupling of the tetramer with [18F]SFB was not successful. Furthermore, labelling of aminooxy-functionalized neurotensin(8-13) derivatives using 4-[18F]fluorobenzaldehyde ([18F]FBA) was investigated. High yields were obtained for the dimer whilst coupling of the tetramer only gave low yields.
In contrast to these findings, labelling of sulfhydryl-functionalized
neurotensin(8-13) derivatives using the maleinimide 4-[18F]fluorobenzaldehyde O-[6-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-hexyl]-oxime ([18F]FBAM) resulted in high radiochemical yields for both, the dimer and the tetramer. Therefore, [18F]FBAM seems to be the most suitable 18F-labelling agent for multivalent neurotensin(8-13) derivatives.


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Publ.-Id: 8956