Positron emission tomography of type 2 cannabinoid receptors for detecting inflammation in the central nervous system

Acta Pharmacol Sin. 2019 Mar;40(3):351-357. doi: 10.1038/s41401-018-0035-5. Epub 2018 Jun 19.

Abstract

Cannabinoid receptor CB2 (CB2R) is upregulated on activated microglia and astrocytes in the brain under inflammatory conditions and plays important roles in many neurological diseases, such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. The advent of positron emission tomography (PET) using CB2R radiotracers has enabled the visualization of CB2R distribution in vivo in animal models of central nervous system inflammation, however translation to humans has been less successful. Several novel CB2R radiotracers have been developed and evaluated to quantify microglial activation. In this review, we summarize the recent preclinical and clinical imaging results of CB2R PET tracers and discuss the prospects of CB2R imaging using PET.

Keywords: cannabinoid receptor CB2; inflammation; microglia; neurological diseases; positron emission tomography.

Publication types

  • Review

MeSH terms

  • Animals
  • Brain / metabolism
  • Central Nervous System Diseases / diagnosis*
  • Humans
  • Inflammation / diagnosis*
  • Positron-Emission Tomography
  • Radiopharmaceuticals / metabolism
  • Receptor, Cannabinoid, CB2 / metabolism*

Substances

  • Radiopharmaceuticals
  • Receptor, Cannabinoid, CB2