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In vivo occupancy of striatal and temporal cortical D2/D3 dopamine receptors by typical antipsychotic drugs

[123I]-epidepride single photon emission tomography (SPET) study

Published online by Cambridge University Press:  03 January 2018

Valeria Bigliani*
Affiliation:
Institute of Psychiatry, London
Rachel S. Mulligan
Affiliation:
Institute of Nuclear Medicine, University College London Medical School, London
Paul D. Acton
Affiliation:
Institute of Nuclear Medicine, University College London Medical School, London
Dimitris Visvikis
Affiliation:
Institute of Nuclear Medicine, University College London Medical School, London
Peter J. Ell
Affiliation:
Institute of Nuclear Medicine, University College London Medical School, London
Caroline Stephenson
Affiliation:
Institute of Psychiatry, London
Robert W. Kerwin
Affiliation:
Institute of Psychiatry, London
Lyn S. Pilowsky
Affiliation:
Institute of Psychiatry, London
*
Dr L. Pilowsky, Institute of Psychiatry, De Crespigny Park, Denmark Hill, London SE5 8AF. Fax: 0171-701 9044; e-mail: [email protected]

Abstract

Background

The dopamine hypothesis proposes that antipsychotic drugs act primarily through limbic cortical D2/D2-like dopamine receptor blockade.

Aim

To evaluate this hypothesis with the D2/D3-selective SPET probe [123I]-epidepride.

Method

[123I]-epidepride SPETscans were performed on 12 patients with schizophrenia treated with antipsychotics and 11 age-matched healthy controls. [123I]-epidepride specific binding to D2/D3 dopamine receptors was estimated, and relative percentage D2/D3 receptor occupancy by typical antipsychotic drugs determined.

Results

Mean (s.d.) daily dose was 669.12 (516.8) mg chlorpromazine equivalents. Mean percentage D2/D3 receptor occupancy was 81.6 (8.1) and 73.2 (13.9) in the temporal cortex and striatum respectively.

Conclusions

Typical antipsychotic drug treatment is associated with substantial temporal cortical D2/D3 receptor occupancy. The relationship between this and efficacy is poor in patients with treatment-resistant schizophrenia.

Type
Papers
Copyright
Copyright © 1999 The Royal College of Psychiatrists 

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