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Gavish, M. Bachman, I., Shoukrun, R., Katz, Y., Veenman, L., Weisinger, G. and Weizman, W. (1999) Enigma of the Peripheral Benzodiazepine Receptor. Pharmacological Reviews, 51, 629-650.

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• TITLE: Activated Microglia in the Brain: Mitochondrial and Cell Membrane-Associated Targets for Positron Emission Tomography

  AUTHORS: Margit Pissarek

  KEYWORDS: Microglia, Inflammation, Brain, PET, TSPO, CX3CR1, Folate Receptor

  JOURNAL NAME: World Journal of Neuroscience, Vol.8 No.1, January 31, 2018

  ABSTRACT: The emission tomographic imaging of activated microglia in the brain moves into the focus of neuroscientific research with increasing recognition of contributions of early inflammatory processes to neurodegenerative, traumatic, cancerous and infectious diseases of the brain. Whereas the mitochondrial isoform of the 18 kDa translocator protein (TSPO1) has been the main cellular target for positron emission tomography (PET) of this type of cells for decades, alternative marker proteins in the plasma membrane of microglia challenge efforts in ligand development, recently. The present report includes PET approaches using the chemokine receptor CX3CR1 and the FR2 folate receptor in parallel to small molecule PET tracers available for in vivo visualization of the “classical” target TSPO1. It compares first and second generation of TSPO1 ligands as well as new compounds like the tetrahydrocarbazole [18F]GE-180 and the quinazoline [11C]ER176 presumed to reduce polymorphism-related inter-subject variations, with allosteric ligands for the chemokine receptor CX3CR1 and with radio labelled folate conjugates targeting the folate “cargo” receptor FR1 and the FR2 receptor characteristic for anti-inflammatory M2 microglia.