Essential Principles and Recent Progress in the Development of TSPO PET Ligands for Neuroinflammation Imaging.

ABSTRACT: The translocator protein 18kDa (TSPO) is expressed in the outer mitochondrial membrane and is implicated in several functions, including cholesterol transport and steroidogenesis. Under normal physiological conditions, TSPO is present in very low concentrations in the human brain but is markedly upregulated in response to brain injury and inflammation. This upregulation is strongly associated with activated microglia. Therefore, TSPO is particularly suited for assessing active gliosis associated with brain lesions following injury or disease. For over three decades, TSPO has been studied as a biomarker. Numerous radioligands for positron emission tomography (PET) that target TSPO have been developed for imaging inflammatory progression in the brain. Although [¹¹C]PK11195, the pr

SUBMITTER: Viviano M 

PROVIDER: S-EPMC10080361 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature