Comparison of in vivo dopamine D2 receptor binding of [(123)I]AIBZM and [(123)I]IBZM in rat brain

Nucl Med Biol. 2001 May;28(4):383-9.

Abstract

[(123)I]AIBZM, (S)-5-[(123)I]-Iodo-N-[(1-ethyl-2-pyrrolidinyl)]methyl-4-amine-2-methoxybenzamide is a derivative with high affinity for the D2 receptor. Labeling was achieved by the Iodogen method. The in vivo affinity for the D2 receptor and the biological characteristics were performed in rats. The brain uptake of [(123)I]AIBZM was significantly lower, however the striatum/cerebellum ratio (2h p.i.) was higher than that of [(123)I]IBZM. Because of the high affinity and its possibly lower unspecific binding compared to [(123)I]IBZM, [(123)I]AIBZM may be a potential imaging agent for the D2 dopamine receptor.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Autoradiography
  • Benzamides / pharmacokinetics*
  • Blood Proteins / metabolism
  • Brain / diagnostic imaging*
  • Brain Chemistry
  • Chemical Phenomena
  • Chemistry, Physical
  • Protein Binding
  • Pyrrolidines / pharmacokinetics*
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D2 / metabolism*
  • Tissue Distribution

Substances

  • 5-iodo-N-((1-ethyl-2-pyrrolidinyl))methyl-4-amine-2-methoxybenzamide
  • Benzamides
  • Blood Proteins
  • Pyrrolidines
  • Radiopharmaceuticals
  • Receptors, Dopamine D2
  • 3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide