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Radioligands for positron emission tomography imaging of cannabinoid type 2 receptor
Author(s) -
Spinelli Francesco,
Mu Linjing,
Ametamey Simon M.
Publication year - 2018
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3579
Subject(s) - radioligand , cannabinoid receptor type 2 , cannabinoid receptor , cannabinoid , neuroprotection , positron emission tomography , chemistry , receptor , preclinical imaging , in vivo , downregulation and upregulation , neuroscience , pharmacology , medicine , biology , biochemistry , agonist , microbiology and biotechnology , gene
The cannabinoid type 2 (CB2) receptor is an immunomodulatory receptor mainly expressed in peripheral cells and organs of the immune system. The expression level of CB2 in the central nervous system under physiological conditions is negligible, however under neuroinflammatory conditions an upregulation of CB2 protein or mRNA mainly colocalized with activated microglial cells has been reported. Consequently, CB2 agonists have been confirmed to play a role in neuroprotective and anti‐inflammatory processes. A suitable positron emission tomography radioligand for imaging CB2 would provide an invaluable research tool to explore the role of CB2 receptor expression in inflammatory disorders. In this review, we provide a summary of so far published CB2 radioligands as well as their in vitro and in vivo binding characteristics.