WAY-351812 is a selective and potent agonist of the GPR139 receptor, which is an orphan G-protein-coupled receptor expressed primarily in the brain, especially in regions associated with motor control and reward processing such as the striatum and hypothalamus. Due to its selectivity, it is widely used in neuroscience research to probe the physiological and pathological roles of GPR139. One major application of WAY-351812 is in studying the modulation of dopaminergic and glutamatergic neurotransmission. Activation of GPR139 by WAY-351812 has been linked to changes in neuronal activity that may influence behaviors related to addiction, depression, and schizophrenia. Researchers use it to explore potential therapeutic targets for neuropsychiatric disorders, particularly where monoaminergic systems are dysregulated. It is also employed in preclinical studies to assess the effects of GPR139 activation on hormone release, including adrenocorticotropic hormone (ACTH) and thyroid-stimulating hormone (TSH), suggesting a role in neuroendocrine regulation. Its use in animal models helps determine the receptor’s involvement in metabolic and stress-related pathways. Because GPR139 is still an emerging target, WAY-351812 serves as a critical tool compound for validating the receptor’s function and evaluating its potential as a drug target. It enables pharmacological profiling and helps design more advanced ligands for possible clinical development.