Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf
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86Y-labelled L RNA oligonucleotides as Molecular Probes for Positron Emission Tomography (PET)Schlesinger, J.; Bergmann, R.; Klußmann, S.; Wüst, F.; Pietzsch, H.-J.
A short 5-aminohexyl-functionalised L RNA oligonucleotide 1 (sequence: UGA CUG ACU GAC 3, MW 3975) was used to study the influence of two different 86Y DOTA chelates on the biodistribution in Wistar rats. The L-oligonucleotide 1 was conjugated with 1,4,7,10 tetraazacyclododecane-N,N,N,N-tetraacetic acid (DOTA) using N-succinimide ester (DOTA-NHS) 2 and isothiocyanate derivative (p SCN bz DOTA) 4 to afford the corresponding amide 3 and thiourea 5, respectively. Both DOTA-functionalised L RNA oligonucleotides 3 and 5 were labelled with the medium half-life positron-emitting radiometal 86Y (t1/2 = 14.7 h) in 76 % and 85 % radiochemical yield. 86Y-Complexes 3a and 5a represent the first examples of L-oligonucleotides labelled with the positron emitter 86Y.
The in vivo biodistribution of 86Y-complex 3a showed a faster elimination from the body via the kidneys compared to thiourea-containing 86Y-complex 5a. Transient accumulation of radioactivity in the kidneys and the adrenals was found for both 86Y-complexes 3a and 5a. After incubation of 86Y-complex 5a in whole rat blood at 37°C no noticeable decomposition could be observed over 12 h as confirmed by HPLC-analysis
7th International Symposium on Technetium in Chemistry and Nuclear Medicine, 06.-09.09.2006, Bressanone, Italy
Contribution to external collection
U.Mazzi: Rhenium and Other Metals in Chemistry and Nuclear Medicine, Padova: SGEditoriali, 2006, 88-89884-04-5, 211-214