Synthesis of [11C-methyl]-(-)-OSU6162, its regional brain distribution and some pharmacological effects of (-)-OSU6162 on the dopaminergic system studied in the rhesus monkey by positron emission tomography

Nucl Med Biol. 1997 Aug;24(6):507-11. doi: 10.1016/s0969-8051(97)00023-1.


The labelling of the presynaptic dopamine receptor antagonist (-)-OSU6162, ((S)-(-)-3-(3-(methylsulfonyl)phenyl)-1-propylpiperidine) was performed by an alkylation with [11C]methyl iodide of the thio anion (-)-OSU1281, followed by a selective oxidation to the corresponding methyl sulfone, [11C-methyl]-(-)-OSU6162. The total radiochemical yield calculated from the produced [11C]carbon dioxide to final product was about 25% and the time of synthesis was in the range of 40 min from end of bombardment. The synthesis of the precursor, (-)-OSU1281, was performed from (-)-3PPP in a three-step synthesis. The regional brain distribution of (-)-OSU6162 radiolabelled with 11C was studied in rhesus monkeys by means of positron emission tomography, PET. [11C-Methyl]-(-)-OSU6162 was rapidly and uniformly distributed to gray matters of the brain, and no decrease of radioactivity uptake in the brain was seen after pretreatment with 1 to 3 mg/kg/h of (-)-OSU6162. The effect of doses of 1 to 3 mg/kg/h of (-)-OSU6162 on the dopamine binding was studied by PET using [11C-methyl]raclopride. Radioactivity in the striatum was significantly and dose-dependently decreased by (-)-OSU6162 (r = 0.88), supporting competition with dopamine for selective binding to dopamine receptors.

MeSH terms

  • Animals
  • Brain / metabolism*
  • Carbon Radioisotopes
  • Dopamine / metabolism*
  • Dopamine Antagonists / chemical synthesis*
  • Dopamine Antagonists / pharmacokinetics
  • Dopamine Antagonists / pharmacology
  • Female
  • Macaca mulatta
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacokinetics
  • Piperidines / pharmacology
  • Raclopride
  • Salicylamides / metabolism
  • Tomography, Emission-Computed*


  • Carbon Radioisotopes
  • Dopamine Antagonists
  • Piperidines
  • Salicylamides
  • OSU 6162
  • Raclopride
  • Dopamine