Ro 61-8048 is primarily used in neuroscience research as a selective and potent inhibitor of kynurenine 3-monooxygenase (KMO), an enzyme in the kynurenine pathway of tryptophan metabolism. By inhibiting KMO, it shifts the metabolic flux away from the neurotoxic branch of the pathway that produces metabolites like 3-hydroxykynurenine and quinolinic acid, which are implicated in neuroinflammation and excitotoxicity. This makes Ro 61-8048 a valuable tool for studying neurodegenerative conditions such as Huntington’s disease, Alzheimer’s disease, and Parkinson’s disease, where dysregulation of the kynurenine pathway is observed.

It has also been investigated for its potential to modulate immune responses and neuroprotection in animal models, particularly in contexts involving inflammation-driven neurological dysfunction. Due to its ability to cross the blood-brain barrier, Ro 61-8048 allows for central nervous system targeting, enhancing its utility in preclinical studies aimed at understanding the role of kynurenine metabolism in behavior, psychiatric disorders, and neuroprotection. Its application remains largely experimental and confined to research settings.