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The GPR52 agonist program at the Warren Center for Neuroscience Drug Discovery (WCNDD) is focused on the development of small-molecule agonists targeting the orphan G-protein coupled receptor 52 (GPR52). GPR52 is highly expressed in the medial prefrontal cortex and on dopamine D2 receptor-expressing medium spiny neurons in the striatum. Activation of GPR52 is hypothesized to provide antipsychotic-like effects and improve cognitive function by modulating dopaminergic and glutamatergic signaling without the side effects associated with direct D2 receptor antagonism. The program is currently in the lead optimization phase, targeting indications such as schizophrenia, Alzheimer's disease, and Parkinson's disease.
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