Imaging Inflammation using PET Radioligands that Target Translocator Protein 18?kDa with High Affinity Regardless of Genotype

This technology includes a group of radioligands that label inflammatory cells specifically, accurately, and across different genotypes and can be detected using Positron Emission Tomography (PET). The radioligands target the Translocator protein 18 kDa (TSPO) receptor which is present on the outer mitochondrial membrane and is involved in the production of steroids. Current TSPO radioligands either lack specificity or have highly variable inter-subject sensitivities due to TSPO genotypic differences. These new ligands permit a simplified interpretation and quantification of the binding signal.

During inflammation of the central nervous system, TSPO levels are increased. Neuroinflammation is symptomatic of many neuropsychiatric and neurodegenerative disorders, such as multiple sclerosis, stroke, epilepsy, dementia, and traumatic brain injuries. Thus, monitoring and quantifying TSPO with radioligands using PET may have clinical application in understanding, diagnosing, and treating many neuropsychiatric disorders.