Radiosynthesis of [F-18] N-3-fluoropropyl-2-beta-carbomethoxy-3-beta-(4-iodophenyl) nortropane and the first human study with positron emission tomography

A procedure for the routine preparation of [F-18]FP-CIT has been developed. Purification of the final product was achieved by preparative HPLC using phenethyl column without decomposition or epimerization. [F-18] labeled-N-fluoropropyl-2 beta-carbomethoxy-3 beta-(4-iodophenyl) nortropane was prepared and PET imaging was performed on human subjects. A high uptake into striatal regions was observed. HPLC plasma analysis using [F-18]FP-CIT indicated the presence of only one metabolite. By directly comparing the behavior of these three radiotracers ([F-18]DOPA, [I-123]FP-CIT, and [F-18]FP-CIT) in the same subjects, we can enhance our understanding of the dopaminergic system as well as the relative potential of these techniques in a clinical research setting. Copyright (C) 1996 Elsevier Science Inc.