EFFICIENT [~18F]FLUORINATION OF HYNIC-[TYR~3]-OCTREOTATE (HYNICTATE) VIA HYDRAZONE FORMATION

摘要

Routine application of [~18F]-labeled ligands for in vivo receptor imaging with PET is limited by the current lack of rapid and high-yield [~18F]-labeling strategies. Here we present a two-step [~18F]-labeling methodology based on the linkage of an aldehyde, p[~18F]fluorobenzaldehyde ([~18F]FB), to a hydrazinonicotinamide (HYNIC) derivatized ligand by hydrazone formation. [~18F]-fluorination via hydrazone formation was optimized using a model peptide and the optimized conditions were applied to the [~18F]-fluorination of HYNIC-[Tyr~3]-octreotate (HYNICTATE) for PET imaging of neuroendocrine tumors.