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Obenaus, E.; Crudo, J.; Edreira, M.; Viaggi, M.; De Castiglia, S.G.
99mTc labelled peptides for imaging of peripheral receptors. Final report of a co-ordinated research project. 1995-19992001
99mTc labelled peptides for imaging of peripheral receptors. Final report of a co-ordinated research project. 1995-19992001
AbstractAbstract
[en] The aim of the present work was to study the biological and radiochemical behaviour of two somatostatin analogues, the RC-160 and Tyr3Octreotide(TOC) peptides when labelling with 99mTc by two methods: direct and indirect using S-benzoyl- mercaptoacetyl triglycine (MAG-3) and hydrazinonicotinamide (HYNIC) as chelating agents. RC-160 was labelled with 125I (30% labelling yield) in order to examine its receptor specificity and to study the biodistribution in normal animals. A total binding of 30% and a non specific binding lower than 10% was obtained. On the other hand, the RC-160 was labelled with 99mTc by a direct method (70% labelling yield), using sodium ascorbate and dithionite in order to reduce the peptide and 99mTc, respectively. The synthesis of RC-160 with S-benzoyl MAG-3 and TOC with HYNIC, for labelling with 99mTc are also described. The conjugates were prepared on a small scale and labelled with the radionuclide using tricine as co-ligands for HYNIC conjugates. Chromatographic studies were performed using HPLC system and radiochemical purities higher than 75% and 95% were obtained respectively. Biodistributions studies in normal Wistar rats were performed and results were correlated with chromatographic and protein binding properties. Lower lipophilicity of the labelled conjugates resulted in a higher renal excretion. HYNIC-TOC complex showed promising results when labelling with 99mTc using tricine as co-ligand although higher stability should be found for ternary co-ligands compared to tricine. (author)
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International Atomic Energy Agency, Vienna (Austria); 183 p; ISSN 1011-4289;
; Apr 2001; p. 17-27; 11 refs, 13 figs

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Report
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BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, HOURS LIVING RADIOISOTOPES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, KINETICS, MEMBRANE PROTEINS, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, PROCESSING, PROTEINS, RADIOISOTOPES, SEPARATION PROCESSES, TECHNETIUM ISOTOPES, USES, YEARS LIVING RADIOISOTOPES
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