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Molecular imaging of microglia/macrophages in the brain

Neuroinflammation perpetuates neuronal damage in many neurological disorders. Activation of resident microglia and infiltration of monocytes/macrophages contributes to neuronal injury and synaptic damage. Noninvasive imaging of these cells in vivo provides a means to monitor progression of disease as well as assess efficacies of potential therapeutics. This review provides an overview of positron emission tomography (PET) and magnetic resonance (MR) imaging of microglia/macrophages in the brain. We describe the rationale behind PET imaging of microglia/macrophages with ligands that bind to translocator protein‐18 kDa (TSPO). We discuss the prototype TSPO radioligand [11C]PK11195, its limitations, and the development of newer TSPO ligands as PET imaging agents. PET imaging agents for targets other than TSPO are emerging, and we outline the potential of these agents for imaging brain microglia/macrophage activity in vivo. Finally, we briefly summarize advances in MR imaging of microglia/macrophages using iron oxide nanoparticles and ultra‐small super paramagnetic particles that are phagocytosed. Despite many technical advances, more sensitive agents are required to be useful indicators of neuroinflammation in brain. © 2012 Wiley Periodicals, Inc.