Pharmacopsychiatry 2007; 40: S34-S39
DOI: 10.1055/s-2007-990303
Original Paper

© Georg Thieme Verlag KG Stuttgart · New York

On the Effects of Partial Agonists of Dopamine Receptors for the Treatment of Schizophrenia

M. Koch 1
  • 1Department of Neuropharmacology, Brain Research Institute, University of Bremen, Bremen
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Publikationsverlauf

Publikationsdatum:
17. Dezember 2007 (online)

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Abstract

The aim of this paper is to describe the possible effects of antipsychotic drugs on neurotransmitter interactions in cortico-striatal circuits related to schizophrenia symptoms, with special emphasis on the action of partial agonists of dopamine and serotonin receptors.

Partial agonists are characterised by a high affinity and a low intrinsic activity. However, since the intrinsic activity of the ligand-bound receptor is still higher than after antagonist binding, partial agonists can act as agonists or as antagonists, depending on the endogenous levels of dopamine and receptor reserve. Aripiprazole is a partial agonist at dopamine D2-receptors and at serotonin 1A-receptors, and is currently the only marketed drug of this class of agents that is used for the treatment of schizophrenia.