Fully automated peptide radiolabeling from [F-18]fluoride

摘要

The biological properties of receptor-targeted peptides have made them popular diagnostic imaging and therapeutic agents. Typically, the synthesis of fluorine-18 radiolabeled receptor-targeted peptides for positron emission tomography (PET) imaging is a time consuming, complex, multi-step synthetic process that is highly variable based on the peptide. The complexity associated with the radiolabeling route and lack of robust automated protocols can hinder translation into the clinic. A fully automated batch production to radiolabel three peptides (YGGFL, cRGDyK, and Pyr-QKLGNQWAVGHLM) from fluorine-18 using the ELIXYS FLEX/ CHEM (R) radiosynthesizer in a two-step process is described. First, the prosthetic group, 6-[F-18] fluoronicotinyl-2,3,5,6-tetrafluorophenyl ester ([F-18] FPy-TFP) was synthesized and subsequently attached to the peptide. The [F-18] FPy-peptides were synthesized in 13-26% decay corrected yields from fluorine-18 with high molar activity 1-5 Ci mmol(-1) and radiochemical purity of > 99% in an overall synthesis time of 97 +/- 3 minutes.