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

Nucl Med Biol. 1996 Nov;23(8):999-1004. doi: 10.1016/s0969-8051(96)00155-2.

Abstract

A procedure for the routine preparation of [18F]FP-CIT has been developed. Purification of the final product was achieved by preparative HPLC using phenethyl column without decomposition or epimerization. [18F] 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 [18F]FP-CIT indicated the presence of only one metabolite. By directly comparing the behavior of these three radiotracers ([18F]DOPA, [123I]FP-CIT, and [18F]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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Isotope Labeling / methods
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / isolation & purification
  • Tomography, Emission-Computed
  • Tomography, Emission-Computed, Single-Photon
  • Tropanes / chemical synthesis*
  • Tropanes / isolation & purification

Substances

  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Tropanes
  • 2-carbomethoxy-8-(3-fluoropropyl)-3-(4-iodophenyl)tropane