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Project

Preclinical validation and first in man study of PET radioligands for the cannabinoidreceptor type 2.

Different pathologies (among which neurodegenerative diseases, multiple sclerosis, atherosclerosis, acute inflammation) are characterized by an increased expression of the CB2 receptor, which is a target for the development of new analgesic and anti-inflammatory drugs. In vivo visualization of CB2 receptors using positron emission tomography allows to translationally investigate the role of these receptors in vivo and is an important instrument to validate candidate medicines that target CB2 receptors. Previous research in our laboratory identified 4 potential PET radioligands for the visualization of CB2 in brain. This project aims to validate these ligands: (1) In a ratmodel (microPET) with local cerebral increase of CB2 receptors secondary to stereotactic injection of an adeno-associated CB2 vector construct. (2) In a model of peripheral inflammation. These animal models will be used for in vivo binding inhibition studies with exogenous and endogenous cannabinoïds. (3) In volunteers ('first in man' study) to study the dosimetry, metabolisation, kinetic modelling, and test-retest variability of the optimal ligand after conducting the required toxicity tests and drafting an IMPD. The radiosynthesis of fluorine-18 labelled compounds will be optimised and a one step labelling procedure will be developed.
Date:1 Jan 2010 →  31 Dec 2013
Keywords:Neuroinflammation, Cannabinoid type 2 (CB2), Molecular imaging, Positron emission tomography (PET), Radiotracer
Disciplines:Medicinal products