~188Re(III)-'4+l'-MIXED-LIGAND COMPLEXES: STABILITY STUDIES AND LABELING OF BIOMOLECULES

摘要

In order to understand relationships between the structure of rhenium-188 '4+1' complexes and their in vitro stability we synthesized a series of rhenium model complexes and determined their stability in human plasma. Rhenium-188 '4+1' complexes were synthesized using different monodentate phosphorus(III) ligands, including both lipophilic and hydrophilic tertiary phosphines and phosphites (~188Rel-3) and unsubstituted tetradentate ligands and substituted NS3 ligands bearing a carboxyl group or an isopropyl amide were used as chelators (~188Re4-6). As instability in aqueous solution leads always to perrhenate, the amount of ~188ReO_4~ formed after lh, 24 h and 48 h was determined by TLC.