Preliminary Investigation of a Novel 18F Radiopharmaceutical for Imaging CB2 Receptors in a SOD Mouse Model

We successfully radiolabelled a novel prospective cannabinoid type 2 receptor ligand with F-18 and tested its biodistribution in animal models by positron emission tomography (PET)/computed tomography (CT) imaging. The radiolabelling process was conducted on an alkyl mesylate fragment of the main na...

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Bibliographic Details
Published in:Australian journal of chemistry Vol. 74; no. 6; pp. 443 - 452
Main Authors: Pascali, Giancarlo, Panetta, Daniele, De Simone, Mariarosaria, Burchielli, Silvia, Lucchesi, Valentina, Sanguinetti, Elena, Zanoni, Simone, Iozzo, Patricia, Saccomanni, Giuseppe, Manera, Clementina, Salvadori, Piero A.
Format: Journal Article
Language:English
Published: CLAYTON SOUTH Csiro Publishing 01.01.2021
CSIRO
Subjects:
Amyotrophic lateral sclerosis
Brain research
Chemistry
Chemistry, Multidisciplinary
Computed tomography
Fluorine isotopes
Investigations
Medical imaging
Optimization
Physical Sciences
Positron emission
Radiochemistry
Radiolabelling
Receptors
Science & Technology
Tomography
GRAPHICAL ANALYSIS
LIGANDS
FLEXIBILITY
HEALTHY
DERIVATIVES
BINDING
PET
RATIONAL DESIGN
ISSN:0004-9425, 1529-5036, 1445-0038
Online Access:Get full text
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Summary:We successfully radiolabelled a novel prospective cannabinoid type 2 receptor ligand with F-18 and tested its biodistribution in animal models by positron emission tomography (PET)/computed tomography (CT) imaging. The radiolabelling process was conducted on an alkyl mesylate fragment of the main naphthyridine core, using highly efficient microfluidic technology. No preliminary protection was needed, and the product was purified by semi-prep HPLC and SPE formulation, allowing the desired diastereomeric mixture to be obtained in 29% radiochemical yield and >95% radiochemically pure. SOD1(G93A) mice were used as model of overexpression of CB2 receptors; PET imaging revealed a significant increase of the tracer distribution volume in the brain of symptomatic subjects compared with the asymptomatic ones.
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ISSN:0004-9425
1529-5036
1445-0038
DOI:10.1071/CH20247