Synthesis of [18F]fluoroalanine and [18F]fluorotamoxifen for imaging breast tumors

J Drug Target. 1993;1(3):259-67. doi: 10.3109/10611869308996084.

Abstract

To develop ligands for imaging breast tumors, [18F]fluoro analogue of tamoxifen and [18F]fluoroalanine were radiosynthesized. In vivo biodistribution studies were performed in mammary tumor-bearing rats. In studies on the biodistribution of an [18F]fluoro analogue of tamoxifen, tumor uptake decreased when rats were pretreated with diethylstilbestrol (DES), suggesting that tracer uptake in tumors was receptor-mediated. An estrogen receptor assay indicated that tumors have a receptor density of 7.5 fmol/mg protein. Studies of the distribution of [18F]fluoroalanine in tissue showed that the tumor-to-tissue ratio increases as a function of time. Positron emission tomography (PET) images of tumor-bearing rats demonstrated that tumors can be visualized 1 h after rats are injected with an [18F]fluoro analogue of tamoxifen. PET imaging of pigs after injection of 10 mCi of [18F]fluoro analogue of tamoxifen showed uterine uptake that could be blocked by DES (50 mg). The findings suggest that both radiotracers are useful for imaging breast tumors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alanine / analogs & derivatives*
  • Alanine / chemical synthesis
  • Animals
  • Cell Transplantation
  • Diethylstilbestrol / pharmacology
  • Female
  • Fluorine Radioisotopes
  • Magnetic Resonance Spectroscopy
  • Mammary Neoplasms, Experimental / diagnostic imaging*
  • Ovary / diagnostic imaging
  • Rats
  • Rats, Inbred F344
  • Receptors, Estrogen / metabolism
  • Swine
  • Tamoxifen / analogs & derivatives*
  • Tamoxifen / chemical synthesis
  • Tissue Distribution
  • Tomography, Emission-Computed
  • Tumor Cells, Cultured
  • Uterus / diagnostic imaging

Substances

  • Fluorine Radioisotopes
  • Receptors, Estrogen
  • Tamoxifen
  • 3-fluoroalanine
  • Diethylstilbestrol
  • 4-fluorotamoxifen
  • Alanine