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Roluperidone is a small molecule investigational drug developed primarily for the treatment of negative symptoms in schizophrenia. It acts as an antagonist at serotonin 5-HT2A receptors, sigma 2 receptors, and alpha 1A adrenergic receptors (with lesser activity at alpha 1B). These targets are implicated in mood regulation, cognition, sleep, anxiety control, movement control, and memory. Roluperidone was designed to avoid direct dopaminergic receptor blockade—differentiating it from many existing antipsychotics—while aiming to address both negative symptoms and cognitive impairment in schizophrenia without typical antipsychotic side effects. Preclinical data suggest that roluperidone may also increase brain-derived neurotrophic factor (BDNF), supporting neurogenesis and synaptic plasticity[1][5][7][10].
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