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DOI: 10.1055/s-2007-990303
© Georg Thieme Verlag KG Stuttgart · New York
On the Effects of Partial Agonists of Dopamine Receptors for the Treatment of Schizophrenia
Publikationsverlauf
Publikationsdatum:
17. Dezember 2007 (online)
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.
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Correspondence
M. Koch
Department of Neuropharmacology
Brain Research Institute
University of Bremen
POB 330440
28334 Bremen
Germany
Telefon: +421/218/72 78
Fax: +421/218/49 32
eMail: Michael.Koch@Uni-Bremen.de