Quantitative ex vivo and in vitro receptor autoradiography using 11C-labeled ligands and an imaging plate: a study with a dopamine D2-like receptor ligand [11C]nemonapride

Nucl Med Biol. 1999 Apr;26(3):291-6. doi: 10.1016/s0969-8051(98)00115-2.

Abstract

Ex vivo and in vitro autoradiography (ARG) with radioluminography is a useful technique to characterize newly developed 11C-labeled positron emission tomography (PET) tracers and to apply them to biological and pharmacological studies. In this report, we have described a method of evaluating the radioactivity distribution quantitatively in ex vivo and in vitro ARG using imaging plates and a dopamine D2-like receptor ligand [11C]nemonapride as a model compound. The photo-stimulated luminescence (PSL) values of the rat brain section provided by the imaging plates showed an excellent linear relationship with the radioactivity in a wide range under constant slice-thickness, although the PSL values slightly decreased with increasing slice-thickness both in ex vivo and in vitro ARG. The injection dose of 11C-tracers for ex vivo ARG was also discussed. We found saturable binding sites of [11C]nemonapride in the cortex besides the striatum both ex vivo and in vitro.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Autoradiography
  • Benzamides / metabolism*
  • Benzamides / pharmacokinetics
  • Binding Sites
  • Brain / diagnostic imaging*
  • Brain / metabolism*
  • Carbon Radioisotopes*
  • Cerebral Cortex / diagnostic imaging
  • Cerebral Cortex / metabolism
  • Corpus Striatum / diagnostic imaging
  • Corpus Striatum / metabolism
  • Dopamine Antagonists / metabolism*
  • Dopamine Antagonists / pharmacokinetics
  • Ligands
  • Luminescent Measurements
  • Male
  • Radiopharmaceuticals / metabolism*
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Rats, Wistar
  • Receptors, Dopamine D2 / metabolism*
  • Tomography, Emission-Computed

Substances

  • Benzamides
  • Carbon Radioisotopes
  • Dopamine Antagonists
  • Ligands
  • Radiopharmaceuticals
  • Receptors, Dopamine D2
  • nemonapride