SYNTHESIS AND STUDY OF LEBELLING METHODS USING RADIONUCLIDES EMITTING OR/AND RADIATION -STUDY OF A SERIES OF PEPTIDES ANALOGUE OF BOMBESIN (bn) USED IN THE DIAGNOSIS AND THERAPY OF TUMOURS

摘要

Among peptides attracting the international scientific interest in the application of their radio-labelled derivatives applied in nuclear medicine for the depiction/therapy of primary and metastatictumours are also included various derivatives of Bombesin (BN). The present invention concerns the design, the synthesis and the study of labelling, with Tc-99m, Re-188, R-186, Sm-153, Lu-177, Y-90, Ga-67, Ga-68 etc radionuclides, the study of a series of peptide derivatives of Bombesin as well as the identification of the structure of the complexes formed by peptides and radio-metals. The invention comprises the design of each peptide, the synthesis, the cleaning, and the identification thereof by aminoacid analysis, its characterization with mass spectrometry and the study of the structure of the complexes formed with radio-metals, by the formation and analysis of respective non radioactive complexes of the stable R-185 element. The applicable synthesis and cleaning methods permit the acquisition of a clean product characterised by the foreseen aminoacid content. Furthermore, the invention comprises the methodology for the lebelling of new peptide derivatives via different radionuclides, the comparative study between radiochemical behaviour and in-vitro stability of the labelled derivatives with analytic techniques and the identification of the structure of the formed complexes via their complexation with Re-185.