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Related Experiment Video

Updated: Jul 14, 2026

Developing a Rat Model for Bipolar Disorder

Developing a Rat Model for Bipolar Disorder

Published on: May 2, 2025

Aripiprazole acts as a selective dopamine D2 receptor partial agonist.

Martyn Wood¹, Charlie Reavill

¹GlaxoSmithKline, Schizophrenia and Bipolar Neurophysiology and Pharmacology, Psychiatry CEDD, Harlow, Essex, UK.

Expert Opinion on Investigational Drugs

|May 16, 2007

Summary

Aripiprazole effectively treats schizophrenia by selectively acting on dopamine D(2) receptors. This atypical antipsychotic does not significantly impact serotonin 5-HT receptors at therapeutic doses, challenging previous understandings.

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Area of Science:

Pharmacology
Neuroscience
Psychiatry

Background:

Aripiprazole is a key medication for schizophrenia, known for its favorable safety profile.
Its mechanism was thought to involve dopamine D(2) and serotonin 5-HT(1A) partial agonism and 5-HT(2) antagonism.
Recent research questions the role of serotonin in aripiprazole's action.

Purpose of the Study:

To review data on aripiprazole's mechanism of action.
To clarify the role of dopamine and serotonin receptors in its clinical effects.
To determine if aripiprazole acts as a "dopamine- and 5-HT stabiliser".

Main Methods:

Review of published and unpublished pharmacological data.
Analysis of studies investigating aripiprazole's receptor binding and activity.
Evaluation of evidence concerning its effects at therapeutic doses.

Main Results:

Aripiprazole functions as a selective partial agonist at dopamine D(2) receptors.
Evidence suggests aripiprazole does not significantly affect serotonin 5-HT receptors at therapeutic doses.
The "dopamine- and 5-HT stabiliser" classification may not fully represent its action.

Conclusions:

Aripiprazole's primary mechanism involves selective D(2) partial agonism.
Serotonin receptor interactions are likely minimal at clinical doses.
This finding refines the understanding of aripiprazole's pharmacological profile in treating schizophrenia.