Striatal and extra-striatal D2/D3 dopamine receptor occupancy by quetiapine in vivo: [123I]-epidepride single photon emission tomography(SPET) study

BackgroundSelective action at limbic cortical dopamine D2-like receptors could mediate atypical antipsychotic efficacy with few extrapyramidal side-effects.AimsTo test the hypothesis that quetiapine has ‘limbic selective’ D2/D3 receptor occupancy in vivo.MethodThe high-affinity D2/D3 ligand [123I]-e...

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Published inBritish journal of psychiatry Vol. 177; no. 5; pp. 408 - 415
Main Authors STEPHENSON, C. M. E, BIGLIANI, V, JONES, H. M, MULLIGAN, R. S, ACTON, P. D, VISVIKIS, D, ELL, P. J, KERWIN, R. W, PILOWSKY, L. S
Format Journal Article
LanguageEnglish
Published London RCP 01.11.2000
Cambridge University Press
Subjects
Affinity
Alcohol
Antidepressants
Antipsychotics
Clozapine
Cortex
Dopamine
Dopamine D2 receptors
Dopamine D3 receptors
Drug dosages
Efficacy
Embargoes & blockades
Emissions
Extrapyramidal system
Laboratories
Medical screening
Neostriatum
Occupancy
Photon emission tomography
Psychiatry
Psychotropic drugs
Quetiapine
Schizophrenia
Scholarships & fellowships
Side effects
Single photon emission computed tomography
Single photon emission tomography
Substance abuse treatment
Temporal lobe
Tomography
United Kingdom > UK
United States > US
Finland
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Summary:BackgroundSelective action at limbic cortical dopamine D2-like receptors could mediate atypical antipsychotic efficacy with few extrapyramidal side-effects.AimsTo test the hypothesis that quetiapine has ‘limbic selective’ D2/D3 receptor occupancy in vivo.MethodThe high-affinity D2/D3 ligand [123I]-epidepride and single photon emission tomography were used to estimate D2/D3 specific binding and an index of relative percentage D2/D3 occupancy in striatal and temporal cortical regions for quetiapine-treated patients (n=6). Quetiapine-, and previously studied typical-antipsychotic- and clozapine-treated patients were compared.ResultsMean (s.d.) relative percentage D2/D3 receptor occupancy by quetiapine was 32.0% (14.6) in striatum and 60.1% (17.2) in temporal cortex (mean daily dose 450 mg: range 300–700 mg/day). Quetiapine treatment resulted in limbic selective D2/D3 blockade similar to clozapine and significantly higher than typical antipsychotics.ConclusionsPreliminary data suggest that limbic selective D2/D3 receptor blockade is important for atypical drug action.
ISSN:0007-1250
1472-1465
DOI:10.1192/bjp.177.5.408