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RESEARCH PRODUCT

Die nächste Generation „atypischer” Antipsychotika: Der Beitrag der Positronenemissionstomographie

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Almost fifteen years of research with Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) have led to a profound understanding of the relationships between antipsychotic doses and plasma levels on the one hand and occupancy of (striatal) D 2 -like dopamine receptors on the other hand as well as with the associated clinical effects and side effects. Furthermore, with the development of clinically atypical" antipsychotics PET studies helped to generate hypotheses regarding the essential pharmacological properties of this heterogeneous class of drugs. Possible mechanisms of action include combined D 2 -/5-HT 2 antagonism, preferential mesolimbic binding, and fast dissociation from the D 2 -receptor. Our recently published PET study on the in vivo characterization of the partial dopamine receptor agonist, aripiprazole, suggests a novel mechanism of action, which leads to clinically atypical" properties of an antipsychotic. Aripiprazole, of which the antipsychotic efficacy has been proven in various multicenter clinical trials, leads to almost complete saturation of D 2 -like dopamine receptors at clinically used doses; however, the incidence of extrapyramidal side effects under aripiprazole is not higher than under placebo. PET like no other method is suitable to display in vivo a novel mechanism of atypicality" of a new class of antipsychotics.