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Radioligands for positron emission tomography imaging of cannabinoid type 2 receptor


Spinelli, Francesco; Mu, Linjing; Ametamey, Simon M (2018). Radioligands for positron emission tomography imaging of cannabinoid type 2 receptor. Journal of Labelled Compounds and Radiopharmaceuticals, 61(3):299-308.

Abstract

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.

Abstract

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.

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Additional indexing

Item Type:Journal Article, refereed, further contribution
Communities & Collections:04 Faculty of Medicine > University Hospital Zurich > Clinic for Nuclear Medicine
Dewey Decimal Classification:610 Medicine & health
Uncontrolled Keywords:Organic Chemistry, Analytical Chemistry, Spectroscopy, Biochemistry, Drug Discovery, Radiology Nuclear Medicine and imaging
Language:English
Date:March 2018
Deposited On:08 Feb 2018 20:06
Last Modified:19 Aug 2018 13:55
Publisher:Wiley-Blackwell Publishing, Inc.
ISSN:0362-4803
OA Status:Closed
Publisher DOI:https://doi.org/10.1002/jlcr.3579
PubMed ID:29110331

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