Biodistribution study of [(123)I] ADAM in mice: correlation with whole body autoradiography

Nucl Med Biol. 2002 Aug;29(6):643-50. doi: 10.1016/s0969-8051(02)00323-2.

Abstract

Iodine-123 labeled 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine ([(123)I] ADAM) has been suggested as a promising serotonin transporter (SERT) imaging agent. Much research has been accomplished, mainly focusing on the SERT binding sites in the central nervous system (CNS). However, the biodistribution of [(123)I] ADAM using whole body autoradiography (WBAR) has never been previously described, to the best of our knowledge. In this study, we assayed the biodistribution of [(123)I] ADAM in tissues/organs removed from mice, and measured their radioactivity with a scintillation counter (SC). The results showed that the liver has the highest uptake. On the other hand, the WBAR clearly demonstrated that [(123)I] ADAM was bound to SERT-rich sites including those in the brain stem, lung, adrenal glands and intestinal mucosa. This radiotracer also accumulated in the liver, kidney, and thyroid. The results from both methods were compared; each has its own complementary role in the biodistribution studies. The SC method revealed the total amount of radiotracer accumulation in each organ, and the WBAR demonstrated more anatomical details of the radiotracer's distribution. The whole body distribution results of the radioligand using both methods explore the usage of this novel radioligand for most possible SERT binding sites, not only in the CNS but also in the peripheral nervous system and neuroendocrine tissues. These findings suggest that [(123)I] ADAM is a potentially useful imaging agent for SERT.

Publication types

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

MeSH terms

  • Animals
  • Autoradiography / methods*
  • Biomarkers
  • Carrier Proteins / metabolism*
  • Cinanserin / analogs & derivatives*
  • Cinanserin / pharmacokinetics*
  • Iodine Radioisotopes / pharmacokinetics*
  • Male
  • Membrane Glycoproteins / metabolism*
  • Membrane Transport Proteins*
  • Mice
  • Mice, Inbred ICR
  • Nerve Tissue Proteins*
  • Radiopharmaceuticals / pharmacokinetics
  • Reproducibility of Results
  • Sensitivity and Specificity
  • Serotonin Plasma Membrane Transport Proteins
  • Statistics as Topic
  • Tissue Distribution
  • Whole-Body Counting / methods*

Substances

  • 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine
  • Biomarkers
  • Carrier Proteins
  • Iodine Radioisotopes
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Radiopharmaceuticals
  • Serotonin Plasma Membrane Transport Proteins
  • Slc6a4 protein, mouse
  • Cinanserin