Darstellung von radioaktiv markiertem „Luteinising Hormone Releasing Hormone“ als Radiopharmakon für die Radiodiagnostik und Tumortherapie sowie Untersuchungen zum Einsatz von Aktivestern zur Darstellung von DOTA-Peptid-Konjugaten

In this work several radioactive labeled derivates of the hormone LHRH were synthesised. Under optimisation of the reaction parameters an effective and versatile strategy for the synthesis of these derivates was established. The ligands DTPA and DOTA were coupled to LHRH for radiometel labeling. In some cases the coupling was made direct, in other cases linker were used to create a distance between peptide and ligand for a higher affinity to the receptor. The DTPA derivates werde labeled with Indium-111 and werse used for binding studies in a cell model. Due to the sensible chemistry of DOTA no effective radiolabeling could be achived. The target molecules were synthesised but due to the bad labeling yield they could not be tested in the cell model. The new DTPA conjugated substances were tested in a cell model. No specific enrichment in cells bearing the LHRH receptor was observed but an enhanced unspecific enrichment.