On the effects of partial agonists of dopamine receptors for the treatment of schizophrenia.

摘要

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.