© 2000 The Royal College of Psychiatrists
Striatal and extra-striatal D2/D3 dopamine receptor occupancy by quetiapine in vivo
[123I]-epidepride single photon emission tomography(SPET) study
Institute of Psychiatry, London
Institute of Nuclear Medicine, UCL Medical School, Middlesex Hospital, London
Department of Radiology, University of Pennsylvania
Correspondence: C. M. E. Stephenson, c/o L. S. Pilowsky, Department of Psychological Medicine, Section of Neurochemical Imaging, Institute of Psychiatry, De Crespigny Park, Denmark Hill, London SE5 8AF, UK
Declaration of interest C.M.E.S. and H.M.J. were supported by research grants from Astra Zeneca, V.B. by a research grant from Eli Lilly and R.S.M. by a UK Medical Research Council (MRC) Senior Clinical Research Fellowship Award. L.S.P. is a UK MRC Senior Clinical Research Fellow.
Background Selective action at limbic cortical dopamine D2-like receptors could mediate atypical antipsychotic efficacy with few extrapyramidal side-effects.
Aims To test the hypothesis that quetiapine has ‘limbic selective’ D2/D3 receptor occupancy in vivo.
Method The 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.
Results Mean (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.
Conclusions Preliminary data suggest that limbic selective D2/D3 receptor blockade is important for atypical drug action.
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