Comparison of the binding of the irreversible monoamine oxidase tracers, [(11)C]clorgyline and [(11)C]l-deprenyl in brain and peripheral organs in humans

Nucl Med Biol. 2004 Apr;31(3):313-9. doi: 10.1016/j.nucmedbio.2003.10.003.

Abstract

The monoamine oxidase A and B (MAO A and B) radiotracers [(11)C]clorgyline (CLG) and [(11)C]L-deprenyl (DEP) and their deuterium labeled counterparts (CLG-D and DEP-D) were compared to determine whether their distribution and kinetics in humans are consistent with their physical, chemical and pharmacological properties and the reported ratios of MAO A:MAO B in post-mortem human tissues. Irreversible binding was consistently higher for DEP in brain, heart, kidneys and spleen but not lung where CLG >DEP and not in thyroid where there is no DEP binding. The generally higher DEP binding is consistent with its higher enzyme affinity and larger free fraction in plasma while differences in regional distribution for CLG and DEP in brain, heart, thyroid and lungs are consistent with different relative ratios of MAO A and B in humans.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.
  • Validation Study

MeSH terms

  • Adult
  • Brain / diagnostic imaging*
  • Brain / metabolism*
  • Carbon Radioisotopes / pharmacokinetics
  • Clorgyline / pharmacokinetics*
  • Deuterium / pharmacokinetics
  • Enzyme Activation
  • Female
  • Humans
  • Kinetics
  • Male
  • Metabolic Clearance Rate
  • Middle Aged
  • Monoamine Oxidase / metabolism*
  • Monoamine Oxidase Inhibitors / pharmacokinetics
  • Organ Specificity
  • Protein Binding
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics
  • Selegiline / pharmacokinetics*
  • Tissue Distribution

Substances

  • Carbon Radioisotopes
  • Monoamine Oxidase Inhibitors
  • Radiopharmaceuticals
  • Selegiline
  • Deuterium
  • Monoamine Oxidase
  • Clorgyline