Novel synthesis and initial preclinical evaluation of (18)F-[FDG] labeled rhodamine: a potential PET myocardial perfusion imaging agent

Nucl Med Biol. 2015 Oct;42(10):804-8. doi: 10.1016/j.nucmedbio.2015.06.009. Epub 2015 Jun 19.

Abstract

Myocardial perfusion imaging is one of the most commonly performed investigations in nuclear medicine studies. Due to the clinical importance of [(18)F]-fluoro-2-deoxy-D-glucose ([(18)F]-FDG) and its availability in almost every PET center, a new radiofluorinated [(18)F]-FDG-rhodamine conjugate was synthesized using [(18)F]-FDG as a prosthetic group. In a convenient and simple one-step radiosynthesis, [(18)F]-FDG-rhodamine conjugate was prepared in quantitative radiochemical yields, with total synthesis time of nearly 20 min and radiochemical purity of greater than 98%, without the need for HPLC purification, which make these approaches amenable for automation. Biodistribution studies in normal rats at 60 min post-injection demonstrated a high uptake in the heart (>11% ID/g) and favorable pharmacokinetics. Additionally, [(18)F]-FDG-rhodamine showed an extraction value of 27.63%±5.12% in rat hearts. These results demonstrate that [(18)F]-FDG-rhodamine conjugate may be useful as an imaging agent for the positron emission tomography evaluation of myocardial perfusion.

Keywords: FDG; Fluorine-18; Myocardial perfusion imaging; Positron emission tomography; Rhodamine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chemistry Techniques, Synthetic
  • Drug Stability
  • Fluorodeoxyglucose F18 / chemistry*
  • Humans
  • Male
  • Myocardial Perfusion Imaging / methods*
  • Myocardium / metabolism
  • Positron-Emission Tomography / methods*
  • Radiochemistry
  • Rats
  • Rhodamines / chemical synthesis*
  • Rhodamines / chemistry*
  • Rhodamines / pharmacokinetics
  • Tissue Distribution

Substances

  • Rhodamines
  • Fluorodeoxyglucose F18