PK-11195 is primarily used in scientific research as a selective ligand for the translocator protein (TSPO), previously known as the peripheral benzodiazepine receptor. Its applications are significant in neuroimaging studies, where it is employed in positron emission tomography (PET) scans to visualize and quantify TSPO expression in the brain. This is particularly useful in studying neuroinflammation, as TSPO is upregulated in activated microglia and astrocytes, which are key players in inflammatory responses in neurological disorders such as Alzheimer's disease, multiple sclerosis, and traumatic brain injury.

Additionally, PK-11195 is utilized in preclinical research to investigate the role of TSPO in various cellular processes, including mitochondrial function, apoptosis, and steroidogenesis. Its ability to bind TSPO with high affinity makes it a valuable tool for exploring the pathophysiology of diseases associated with mitochondrial dysfunction and inflammation. In cancer research, PK-11195 has been studied for its potential to target TSPO-expressing tumors, providing insights into diagnostic and therapeutic strategies. Overall, PK-11195 serves as a critical compound in advancing our understanding of TSPO-related mechanisms in health and disease.