Aripiprazole acts as a selective dopamine D₂ receptor partial agonist

Abstract

Aripiprazole has made a significant contribution to the treatment of schizophrenia and related disorders with an improved safety and tolerability profile, which has been attributed to its unique pharmacological profile. It has been claimed that partial agonism of the dopamine D₂ and 5-HT_1A receptors and antagonism of the 5-HT₂ receptor contribute to the clinical profile of aripiprazole, a so-called dopamine- and 5-HT stabiliser. However, recent studies have questioned the role of the 5-HT-mediated systems in the mechanism of action of aripiprazole. This report reviews published and unpublished data that suggest that aripiprazole acts as a selective partial agonist at the dopamine D₂ receptor and does not affect 5-HT receptors at therapeutic doses.

Acknowledgements

The authors would like to thank M Newson for help with the aripiprazole and WAY-100635 catalepsy study and K Clarke and C Scott for the unpublished data in Table 1.

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