Radiosynthesis and biological evaluation of a promising sigma(2)-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer

Appl Radiat Isot. 2010 Dec;68(12):2268-73. doi: 10.1016/j.apradiso.2010.06.004. Epub 2010 Jun 15.

Abstract

Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity sigma(2) receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [(18)F]3 and [(125)I]3, respectively. Studies of [(125)I]3 using murine 66 breast tumor membrane homogenates and evaluation of [(18)F]3 and [(125)I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging sigma(2) receptors in breast cancer.

Publication types

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

MeSH terms

  • Animals
  • Breast Neoplasms / diagnosis*
  • Female
  • Fluorine Radioisotopes / metabolism
  • Iodine Radioisotopes / metabolism
  • Ligands
  • Positron-Emission Tomography
  • Rabbits
  • Rats
  • Receptors, sigma / metabolism*
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Fluorine Radioisotopes
  • Iodine Radioisotopes
  • Ligands
  • Receptors, sigma
  • sigma-2 receptor