Lumateperone tosylate (ITI-007) is a multifunctional small molecule acting as a potent 5-HT2A receptor antagonist, a serotonin transporter (SERT) blocker, and a dopamine D2 receptor modulator with presynaptic partial agonism and postsynaptic antagonism. It is utilized in preclinical research for investigating neuropsychiatric disorders, including schizophrenia and mood disorders, in both in vitro and in vivo models.