Extrastriatal and striatal D2 dopamine receptor blockade with haloperidol or new antipsychotic drugs in patients with schizophrenia

• Published in: British journal of psychiatry Vol. 179; no. 6; pp. 503 - 508
• Main Authors: Xiberas, X., Martinot, J. L., Mallet, L., Artiges, E., Loc'h, C., Mazière, B., Paillère-Martinot, M. L.
• Format: Journal Article
• Language: English
• Published: Cambridge, UK Cambridge University Press 01.12.2001; RCP
• Subjects: Amisulpride; Antipsychotics; Basal ganglia; Clozapine; Cortex; Dopamine; Dopamine D2 receptors; Dopamine D3 receptors; Drug dosages; Embargoes & blockades; Emissions; Haloperidol; Medical imaging; Mental disorders; Neostriatum; Olanzapine; Plasma; Positron emission tomography; Psychiatry; Psychotropic drugs; Risperidone; Schizophrenia; Temporal lobe; Thalamus; Tomography; France
• ISSN: 0007-1250; 1472-1465
• DOI: 10.1192/bjp.179.6.503

BackgroundBoth traditional and atypical antipsychotics have been hypothesised to be effective in schizophrenia through limbic and cortical D2 dopamine receptor blockade.AimsTo investigate this hypothesis with the D2/D3-selective positron emission tomography (PET) probe [76Br]-FLB457.MethodPETscans were performed on 6 controls and 18 patients with schizophreniatreated with haloperidol or with risperidone, clozapine, amisulpride or olanzapine.ResultsThe D2 dopamine receptor blockade was high in the temporal cortex with both haloperidol and atypical antipsychotics. The atypicals, however, induced a significantly lower D2 binding index than haloperidol in the thalamus and in the striatum.ConclusionsResults suggest that cortical D2 dopamine receptors are a common target of traditional and atypical antipsychotics for therapeutic action. Higher in vivo binding to the D2 receptors in the cortex than in the basal ganglia is suggested as an indicator of favourable profile for a putative antipsychotic compound.