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Is the 5-HT2-Receptor a Target for Antipsychotic Drug Action? PET Studies on Dopamine (D2 and Serotonin (5-HT2) Receptor Occupancy in Patients and Healthy Subjects

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Book cover PET for Drug Development and Evaluation

Part of the book series: Developments in Nuclear Medicine ((DNUM,volume 26))

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Abstract

Several types of neuroreceptors are of interest with respect to antipsychotic activity, in particular the D2 dopamine, D1 dopamine 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 [1]. The most widely accepted hypothesis of neuroleptic drug action is that antipsychotic effects are mediated by blockade of the dopamine receptors [2–6]. This hypothesis has been supported by consistent findings of high D2 receptor occupancy in PET studies performed in patients treated with antipsychotic drugs [7–9]. We have recently shown a statistically significant relation between antipsychotic effect and D2 receptor occupancy in a controlled clinical study, using raclopride as an antipsychotic [10]. We have also shown that the risk of extrapyramidal side-effects was significantly increased in patients with occupancy above 80% [11]. On the basis of these findings we have suggested that for classical antipsychotics there is a threshold for antipsychotic effect at about 70% D2 receptor occupancy, and a distinct threshold for EPS at about 80% (figure 1).

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Author information

Authors and Affiliations

  1. Karolinska Institute, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S-171 76, Stockholm, Sweden

    Svante Nyberg, Anna-Lena Nordström, Christer Halldin & Lars Farde

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  1. Svante Nyberg
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  2. Anna-Lena Nordström
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  3. Christer Halldin
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  4. Lars Farde
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  1. Hôpital Neuro-cardiologique, Lyon, France

    D. Comar

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© 1995 Springer Science+Business Media Dordrecht

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Nyberg, S., Nordström, AL., Halldin, C., Farde, L. (1995). Is the 5-HT2-Receptor a Target for Antipsychotic Drug Action? PET Studies on Dopamine (D2 and Serotonin (5-HT2) Receptor Occupancy in Patients and Healthy Subjects. In: Comar, D. (eds) PET for Drug Development and Evaluation. Developments in Nuclear Medicine, vol 26. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-0429-6_8

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  • DOI: https://doi.org/10.1007/978-94-011-0429-6_8

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-4191-1

  • Online ISBN: 978-94-011-0429-6

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