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. 2009 Oct 28;29(43):13730-4.
doi: 10.1523/JNEUROSCI.4172-09.2009.

Effects of the antipsychotic risperidone on dopamine synthesis in human brain measured by positron emission tomography with L-[beta-11C]DOPA: a stabilizing effect for dopaminergic neurotransmission?

Hiroshi Ito  1 , Harumasa Takano, Hidehiko Takahashi, Ryosuke Arakawa, Michie Miyoshi, Fumitoshi Kodaka, Masaki Okumura, Tatsui Otsuka, Tetsuya Suhara
Affiliations

Effects of the antipsychotic risperidone on dopamine synthesis in human brain measured by positron emission tomography with L-[beta-11C]DOPA: a stabilizing effect for dopaminergic neurotransmission?

Hiroshi Ito et al. J Neurosci. .

Abstract

Effects of antipsychotic drugs have widely been considered to be mediated by blockade of postsynaptic dopamine D(2) receptors. Effects of antipsychotics on presynaptic functions of dopaminergic neurotransmission might also be related to therapeutic effects of antipsychotics. To investigate the effects of antipsychotics on presynaptic functions of dopaminergic neurotransmission in relation with occupancy of dopamine D(2) receptors, changes in dopamine synthesis capacity by antipsychotics and occupancy of dopamine D(2) receptors were measured by positron emission tomography (PET) in healthy men. PET studies using [(11)C]raclopride and L-[beta-(11)C]DOPA were performed under resting condition and oral administration of single dose of the antipsychotic drug risperidone on separate days. Although occupancy of dopamine D(2) receptors corresponding dose of risperidone was observed, the changes in dopamine synthesis capacity by the administration of risperidone were not significant, nor was the relation between the occupancy of dopamine D(2) receptors and these changes. A significant negative correlation was observed between the baseline dopamine synthesis capacity and the changes in dopamine synthesis capacity by risperidone, indicating that this antipsychotic can be assumed to stabilize the dopamine synthesis capacity. The therapeutic effects of risperidone in schizophrenia might be related to such stabilizing effects on dopaminergic neurotransmission responsivity.

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Figures

Figure 1.
Figure 1.
The uptake rate constant ki indicating the dopamine synthesis capacity for the baseline study and drug challenge study with risperidone in the putamen (A) and caudate (B).
Figure 2.
Figure 2.
The relations between the occupancy of dopamine D2 receptors and the percentage change in ki by drug challenge with risperidone in the putamen (A) and caudate (B).
Figure 3.
Figure 3.
The relations between ki in the baseline study and the percentage changes in ki by drug challenge with risperidone in the putamen (A) and caudate (B).
See this image and copyright information in PMC

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