Brexpiprazole has a low risk of dopamine D₂ receptor sensitization and inhibits rebound phenomena related to D₂ and serotonin 5-HT_2A receptors in rats.

ABSTRACT:

Background

Long-term antipsychotic treatment in patients with schizophrenia can induce supersensitivity psychosis and tardive dyskinesia which is thought to be caused by dopamine D₂ receptor sensitization. We evaluated the effects of brexpiprazole on D₂ receptor sensitivity after subchronic treatment in rats. We also evaluated whether brexpiprazole could suppress enhanced response to D₂ receptors in rats subchronically dosed with another atypical antipsychotic.

Methods

The maximum D₂ receptor density (B_max ) and apomorphine (a D₂ receptor agonist)-induced stereotypy were measured in rats orally dosed with vehicle, haloperidol (1 mg/kg), or brexpiprazole (4 or 30 mg/kg for B_max , 6 or 30 mg/kg for st

SUBMITTER: Amada N 

PROVIDER: S-EPMC7292306 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature