Title: Preclinical evaluation of [(11)C]NE40, a type 2 cannabinoid receptor PET tracer
Authors: Evens, Nele
Vandeputte, Caroline
Coolen, Charlotte
Janssen, Peter
Sciot, Raf
Baekelandt, Veerle
Verbruggen, Alfons
Debyser, Zeger
Van Laere, Koen
Bormans, Guy # ×
Issue Date: Apr-2012
Publisher: Pergamon Press
Series Title: Nuclear Medicine and Biology vol:39 issue:3 pages:389-399
Abstract: INTRODUCTION: Up-regulation of the type 2 cannabinoid receptor (CB(2)R) has been reported in (neuro)inflammatory diseases. In this study, we report the preclinical evaluation of [(11)C]NE40 as positron emission tomography (PET) radioligand for visualization of the CB(2)R. METHODS: The selectivity of NE40 for CB(2)R and its toxicity and mutagenicity were determined. [(11)C]NE40 was evaluated by biodistribution and autoradiography studies in normal rats and a microPET study in normal mice, rats and a rhesus monkey. Specific in vivo binding of [(11)C]NE40 to human CB(2)R (hCB(2)R) was studied in a rat model with hCB(2)R overexpression. RESULTS: [(11)C]NE40 shows specific CB(2)R binding in the spleen and blood of normal rats and high brain uptake in rhesus monkey. [(11)C]NE40 showed specific and reversible binding to hCB(2)R in vivo in a rat model with local hCB(2)R overexpression. CONCLUSIONS: [(11)C]NE40 shows favorable characteristics as radioligand for in vivo visualization of the CB(2)R and is a promising candidate for hCB(2)R PET imaging.
ISSN: 0969-8051
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Research Group for Neurobiology and Gene Therapy
Radiopharmaceutical Research
Nuclear Medicine & Molecular Imaging
Research Group Neurophysiology
Translational Cell & Tissue Research
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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