11C-SCH 39166, a selective ligand for visualization of dopamine-D1 receptor binding in the monkey brain using PET

Psychopharmacology (Berl). 1991;103(2):150-3. doi: 10.1007/BF02244195.

Abstract

The new selective D1-dopamine receptor antagonist SCH 39166 was labelled with the positron emitting isotope 11C and used as ligand for visualization of dopamine-D1 receptor binding in Cynomolgus monkeys by PET. After intravenous administration of the ligand a marked uptake of radioactivity was recorded in the D1-dopamine receptor-rich striatum and neocortex but not in the dopamine receptor-poor cerebellum. The uptake of radioactivity in striatum and neocortex was markedly displaced after the intravenous injection of a high dose of the D1-dopamine receptor antagonist SCH 23390 but not after the 5-HT2 receptor antagonist ketanserine. 11C-SCH 39166 should be a useful tool to explore D1-dopamine receptor characteristics in the living human brain by PET.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antipsychotic Agents*
  • Benzazepines* / pharmacology
  • Brain / anatomy & histology*
  • Brain / metabolism
  • Brain Chemistry / drug effects
  • Ketanserin / pharmacology
  • Ligands
  • Macaca fascicularis
  • Male
  • Receptors, Dopamine / drug effects
  • Receptors, Dopamine / metabolism*
  • Receptors, Dopamine D1
  • Tomography, Emission-Computed

Substances

  • Antipsychotic Agents
  • Benzazepines
  • Ligands
  • Receptors, Dopamine
  • Receptors, Dopamine D1
  • ecopipam
  • Ketanserin