Synthesis and biological evaluation of a fluorine-18 labeled estrogen receptor-alpha selective ligand: [18F] propyl pyrazole triol

Nucl Med Biol. 2003 May;30(4):397-404. doi: 10.1016/s0969-8051(02)00446-8.

Abstract

The two estrogen receptor subtypes, ERalpha and ERbeta, play important roles in breast cancer. To develop an ERalpha imaging agent, we synthesized fluoropropyl pyrazole triol (FPPT, 2), an analog of our ERalpha-selective ligand PPT. FPPT retains the high ERalpha binding selectivity of its parent PPT. We prepared [(18)F]FPPT ((18)F-2) in high specific activity, but estrogen target tissue uptake in female rats was minimal and was not displaceable by unlabeled estradiol, probably because of the lipophilicity and triphenolic nature of FPPT.

Publication types

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

MeSH terms

  • Animals
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Female
  • Fluorine Radioisotopes
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / metabolism
  • Pyrazoles / pharmacokinetics
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / metabolism
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Receptors, Estrogen / metabolism
  • Tissue Distribution

Substances

  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Fluorine Radioisotopes
  • Pyrazoles
  • Radiopharmaceuticals
  • Receptors, Estrogen
  • pyrazole