Journal article
Dopamine D2/3 receptor occupancy by quetiapine in striatal and extrastriatal areas
The international journal of neuropsychopharmacology, Vol.13(7), pp.951-960
08/2010
DOI: 10.1017/S1461145710000374
PMID: 20392299
Abstract
Quetiapine is next to clozapine an antipsychotic agent that exerts hardly any extrapyramidal side-effects at clinical efficacious doses. Some previous receptor occupancy studies reported preferential extrastriatal D2/3 receptor (D2/3R)-binding properties of second-generation antipsychotics and suggested this as possible reason for improved tolerability. This positron emission tomography (PET) investigation was designed to compare the occupancy of dopamine D2/3Rs by quetiapine in striatal and extrastriatal brain regions. Therefore, a cohort of 16 quetiapine-treated psychotic patients underwent an [18F]fallypride (FP) PET scan. Due to the high affinity of FP and its comparatively long half-life, striatal and extrastriatal binding potentials could be determined in one single scan. Receptor occupancy was calculated as percent reduction in binding potential relative to age-matched medication-free patients suffering from schizophrenia. Quetiapine occupied 44±18% in the temporal cortex and 26±17% in the putamen, a difference significant at the level of p=0.005 (Student's t test). Quetiapine showed a mean occupancy of 36±16% and in the thalamus. In the caudate nucleus there was an occupancy of 29±16% (p=0.0072). Individual occupancy levels did not exceed 59% in any of the striatal volumes of interest. The time-interval between scan and last drug ingestion did not influence the relationship between plasma concentration and central D2/3R occupancy. Taken together, quetiapine shows preferential extrastriatal binding at D2/3Rs; the extent of this difference is comparable to that previously described for clozapine. Both antipsychotics show very low affinity for D2/3Rs.
Details
- Title: Subtitle
- Dopamine D2/3 receptor occupancy by quetiapine in striatal and extrastriatal areas
- Creators
- Ingo Vernaleken - 1Department of Psychiatry and Psychotherapy, RWTH Aachen University, Aachen, and JARA-Translational Brain Medicine, GermanyHildegard Janouschek - 1Department of Psychiatry and Psychotherapy, RWTH Aachen University, Aachen, and JARA-Translational Brain Medicine, GermanyMardjan Raptis - 2Department of Nuclear Medicine, RWTH Aachen University, Aachen, GermanySandra Hellmann - 1Department of Psychiatry and Psychotherapy, RWTH Aachen University, Aachen, and JARA-Translational Brain Medicine, GermanyTanja Veselinovic - 1Department of Psychiatry and Psychotherapy, RWTH Aachen University, Aachen, and JARA-Translational Brain Medicine, GermanyAnno Bröcheler - 1Department of Psychiatry and Psychotherapy, RWTH Aachen University, Aachen, and JARA-Translational Brain Medicine, GermanyChristian Boy - 3Department of Nuclear Medicine, University Hospital Essen, Essen, GermanyPaul Cumming - 4Department of Nuclear Medicine, LMU University, Munich, GermanyChristoph Hiemke - 5Department of Psychiatry, University of Mainz, Mainz, GermanyFrank Rösch - 6Institute for Nuclear Chemistry, University of Mainz, Mainz, GermanyWolfgang M Schäfer - 2Department of Nuclear Medicine, RWTH Aachen University, Aachen, GermanyGerhard Gründer - 1Department of Psychiatry and Psychotherapy, RWTH Aachen University, Aachen, and JARA-Translational Brain Medicine, Germany
- Resource Type
- Journal article
- Publication Details
- The international journal of neuropsychopharmacology, Vol.13(7), pp.951-960
- DOI
- 10.1017/S1461145710000374
- PMID
- 20392299
- NLM abbreviation
- Int J Neuropsychopharmacol
- ISSN
- 1461-1457
- eISSN
- 1469-5111
- Publisher
- Cambridge University Press; Cambridge, UK
- Number of pages
- 10
- Language
- English
- Date published
- 08/2010
- Academic Unit
- Psychiatry; Iowa Neuroscience Institute
- Record Identifier
- 9984003964202771
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