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

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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.

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Authors and Affiliations

  1. Department of Psychiatry and Psychology, Karolinska Institute, and the Karolinska Pharmacy, Karolinska Hospital, PO Box 60500, S-10401, Stockholm, Sweden

    L. Farde, C. Halldin, S. Stone-Elander & G. Sedvall

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  1. L. Farde
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  2. C. Halldin
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  3. S. Stone-Elander
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  4. G. Sedvall
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Farde, L., Halldin, C., Stone-Elander, S. et al. PET analysis of human dopamine receptor subtypes using 11C-SCH 23390 and 11C-raclopride. Psychopharmacology 92, 278–284 (1987). https://doi.org/10.1007/BF00210831

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  • DOI: https://doi.org/10.1007/BF00210831

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