Investigations into tumor accumulation and peroxisome proliferator activated receptor binding by F-18 and C-11 fatty acids

Nucl Med Biol. 2002 Feb;29(2):211-6. doi: 10.1016/s0969-8051(01)00300-6.

Abstract

[11C]Acetate, a myocardial PET imaging agent for analysis of oxidative metabolism, has potential use in tumor imaging. Aromatic fatty acids display antitumor effects with phenylacetate currently in clinical trial. Tumor differentiation and cytostasis resulting from phenylacetate treatment may involve the peroxisome proliferator-activated receptor alpha (PPARalpha). To examine whether aromatic fatty acids are potential imaging agents for PPARalpha or tumors in general, [11C]phenylacetic acid (PAA) and [18F]fluorophenyl-acetic acid (FPAA) were synthesized and evaluated in EMT-6 tumor bearing mice and 9L-Glioma tumor bearing rats and compared to [11C]acetate. [11C]Acetate showed better tumor accumulation than PAA or FPAA. The aromatic fatty acids did not directly bind PPARalpha as confirmed by a biodistribution study of PAA in PPARalpha -/- mice.

Publication types

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

MeSH terms

  • Acetates / pharmacokinetics*
  • Animals
  • Carbon Radioisotopes / pharmacokinetics
  • Female
  • Fluorine Radioisotopes / pharmacokinetics
  • Glioma / diagnostic imaging
  • Glioma / metabolism*
  • Kidney / metabolism
  • Liver / metabolism
  • Mammary Neoplasms, Experimental / diagnostic imaging
  • Mammary Neoplasms, Experimental / metabolism*
  • Mice
  • Mice, Inbred BALB C
  • Mice, Transgenic
  • Phenylacetates / pharmacokinetics*
  • Radionuclide Imaging
  • Rats
  • Rats, Inbred F344
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Tissue Distribution
  • Transcription Factors / metabolism*

Substances

  • Acetates
  • Carbon Radioisotopes
  • Fluorine Radioisotopes
  • Phenylacetates
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors
  • 2-(4-fluorophenyl)acetic acid
  • phenylacetic acid