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Original articles| Volume 33, ISSUE 4, P227-235, February 15, 1993

Central D2-dopamine receptor occupancy in relation to antipsychotic drug effects: A double-blind PET study of schizophrenic patients

DOI:https://doi.org/10.1016/0006-3223(93)90288-O
Central D2-dopamine receptor occupancy in relation to antipsychotic drug effects: A double-blind PET study of schizophrenic patients
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      Abstract

      The relationship between central D2-dopamine receptor occupancy and antipsychotic drug effects was examined in a double-blind study. Raclopride was the compound used to induce a selective occupancy of the D2-dopamine receptors. In addition, 11C-labeled raclopride was the radioligand used to measure occupancy by positron emission tomography (PET). Seventeen schizophrenic patients were randomly assigned to one of three parallel groups treated for 4 weeks with daily doses of 2, 6, or 12 mg of raclopride. D2-receptor occupancy was determined by PET at steady-state conditions in 13 patients who completed the study. A statistically significant relationship was demonstrated between antipsychotic effect and degree of D2-receptor occupancy (p < 0.05). Patients with extrapyramidal side effects had significantly 3igher D2-receptor occupancy than those without (p = 0.02). The finding of a relationship between selective occupancy of the D2-dopamine receptors and clinical effects in schizophrenic patients principally provides new support for the dopamine hypothesis of antipsychotic drug action.

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      Article info

      Publication history

      Received in revised form: October 16, 1992
      Received: June 23, 1992

      Footnotes

      ☆This research was supported by grants from Astra Arcus (Sweden), National Institute of Mental Health (RO41205-07); Ulf Lundahl Memorial Foundation, the Swedish Medical Research Council, (B91-21X-09114-03A); the Karolinska Institute, and the Professor Bror Gadelius memorial fund.

      Identification

      DOI: https://doi.org/10.1016/0006-3223(93)90288-O

      Copyright

      © 1993 Published by Elsevier Inc.

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