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Positron Emission Tomography of in-vivo Binding Characteristics of Atypical Antipsychotic Drugs

Review of D2 and 5-HT2 Receptor Occupancy Studies and Clinical Response

Published online by Cambridge University Press:  06 August 2018

Svante Nyberg ,
Yoshifumi Nakashima ,
Anna-Lena Nordström ,
Christer Halldin  and
Lars Farde
Svante Nyberg*
Affiliation:
Department of Clinical Neuroscience, Karolinska Hospital, Stockholm, Sweden
Yoshifumi Nakashima
Affiliation:
Department of Clinical Neuroscience, Karolinska Hospital, Stockholm, Sweden
Anna-Lena Nordström
Affiliation:
Department of Clinical Neuroscience, Karolinska Hospital, Stockholm, Sweden
Christer Halldin
Affiliation:
Department of Clinical Neuroscience, Karolinska Hospital, Stockholm, Sweden
Lars Farde
Affiliation:
Department of Clinical Neuroscience, Karolinska Hospital, Stockholm, Sweden
*
Dr Svante Nyberg, Department of Clinical Neuroscience, Psychiatry and Psychology Section, Karolinska Institute, Karolinska Hospital, S-171 76 Stockholm, Sweden
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Extract

Several types of neuroreceptors are of interest with respect to antipsychotic activity, in particular the D2, D1, and 5-HT2 receptors. Among currently prescribed antipsychotic drugs, some have an affinity for a broad range of neuroreceptors, while others are more selective for the D2 receptor (Hytell et al, 1985). The most widely accepted hypothesis of neuroleptic drug action is that antipsychotic effects are mediated by a blockade of the dopamine receptors (Carlsson & Lindqvist, 1963; van Rossum, 1966; Creese et al, 1976; Seeman et al, 1976; Peroutka & Snyder, 1980). This hypothesis has been supported by consistent findings of high D2 receptor occupancy in positron emission tomography (PET) studies of patients treated with antipsychotic drugs (Farde et al, 1986; Smith et al, 1988; Baron et al, 1989). At the same time, the risk of extrapyramidal side-effects (EPS) seems particularly high in patients with occupancy above 80% (Farde et al, 1992) (Fig. 1).

Type
Research Article
Information
The British Journal of Psychiatry , Volume 168 , Issue S29: Current Issues in the Development of Atypical Antipsychotic Drugs , May 1996 , pp. 40 - 44
Copyright
Copyright © 1996 The Royal College of Psychiatrists 

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