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

• Published in: Current medicinal chemistry Vol. 29; no. 28; p. 4862
• Main Authors: Viviano, Monica, Barresi, Elisabetta, Siméon, Fabrice G, Costa, Barbara, Taliani, Sabrina, Da Settimo, Federico, Pike, Victor W, Castellano, Sabrina
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01.01.2022
• Subjects: Brain - metabolism; Humans; Ligands; Neuroinflammatory Diseases; Positron-Emission Tomography - methods; Receptors, GABA - genetics; Receptors, GABA - metabolism; radioligand; neuroinflammation; drug development; TSPO; diagnostic marker; imaging; PET

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 upr...