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).
Published Version
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