Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A ( K i =1.5 nM) and 5-HT2A ( K i =2.5 nM), and has antagonist activity at 5-HT2B ( K i =0.19 nM), and 5-HT7 ( K i =2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.