Psychopharmacology

, Volume 92, Issue 3, pp 278–284

PET analysis of human dopamine receptor subtypes using 11C-SCH 23390 and 11C-raclopride

  • L. Farde
  • C. Halldin
  • S. Stone-Elander
  • G. Sedvall
Original Investigations

DOI: 10.1007/BF00210831

Cite this article as:
Farde, L., Halldin, C., Stone-Elander, S. et al. Psychopharmacology (1987) 92: 278. doi:10.1007/BF00210831

Abstract

Tracer doses of 11C-SCH 23390 and 11C-raclopride, selective D1-dopamine and D2-dopamine receptor antagonists, respectively, were injected intravenously into three healthy male volunteers and two drug-treated schizophrenic patients. Regional radioactivity in brain and plasma was followed during 1 h by positron emission tomography (PET). After injection of both ligands a high accumulation of radioactivity was observed in the dopamine-rich caudate putamen. Experiments with 11C-SCH 23390, but not 11C-raclopride, showed a conspicuous accumulation of radioactivity also in the neocortex. None of the ligands accumulated in the dopamine-poor cerebellum. Specific binding of 11C-raclopride in the putamen was reduced by more than 80% in schizophrenic patients treated with antipsychotic doses of sulpiride or cis(Z)-flupentixol decanoate. 11C-SCH 23390 binding was slightly reduced in both the cortex and the putamen after treatment with cis(Z)-flupentixol decanoate but not after sulpiride. The results indicate that clinical antipsychotic drug treatment with sulpiride and cis(Z)-flupentixol decanoate causes a substantial blockade of D2-dopamine receptors in the basal ganglia but has only a minor effect on D1-dopamine receptors.

Key words

Positron emission tomography Dopamine receptor subtypes SCH 23390 Raclopride Antipsychotic drug treatment 

Copyright information

© Springer-Verlag 1987

Authors and Affiliations

  • L. Farde
    • 1
  • C. Halldin
    • 1
  • S. Stone-Elander
    • 1
  • G. Sedvall
    • 1
  1. 1.Department of Psychiatry and Psychology, Karolinska Institute, and the Karolinska PharmacyKarolinska HospitalStockholmSweden

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