Radiopharmaceuticals for PET imaging of neuroinflammation

Abstract

Recently, accumulating evidences have revealed that neuroinflammation seems to be the cornerstone of many neurological diseases including stroke, multiple sclerosis, Alzheimer's disease or Parkinson's disease. Neuroinflammation causes neuronal damages by activation of plenty of cells and molecular mediators in diseases involving inflammatory process. We focus on non-invasive molecular imaging of radioligands that target inflammatory cells and molecules involved in neuroinflammation. Indeed, PET is one of the most promising imaging techniques to visualize and quantify neuroinflammation in vivo. We summarize here the potential neuroinflammation imaging targets and corresponding PET radioligands.

Radiosynthesis of a Novel 11C‐Labeled Derivative of 4’‐O‐Methylhonokiol and Its Preliminary Evaluation in an LPS Rat Model of Neuroinflammation

“…Moreover, neuroinflammation is a universal mechanism of neurodegeneration, because regardless of the initial trigger, the activation of glial cells is accompanied by the same type of changes in gene expression and protein activity and is thus a “programmed” reaction . Positron emission tomography (PET) based on operation of biologically active compounds labeled with short‐lived isotopes 11 C (T 1/2 =20.4 min) and 18 F (T 1/2 =109.8 min) provides a non‐invasive and direct method for assessing neuroinflammatory changes in the brain . Recently, significant progress was achieved in the development of PET radiotracers for inflammatory protein targets, including enzymes (translocator protein 18 kDa, glycogen synthase kinase 3, monoamine oxidase‐B, cyclooxygenase), cannabinoid (CB2) and purine (P2X7) receptors .…”