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RESEARCH ARTICLE (Open Access)
Contents Vol 74(6)

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

Giancarlo Pascali https://orcid.org/0000-0001-7919-8416 A B C E , Daniele Panetta C , Mariarosaria De Simone C D , Silvia Burchielli C , Valentina Lucchesi D , Elena Sanguinetti C , Simone Zanoni B , Patricia Iozzo C , Giuseppe Saccomanni D , Clementina Manera D and Piero A. Salvadori C
+ Author Affiliations
- Author Affiliations

A Nuclear Medicine Department, Prince of Wales Hospital, Barker Street, Randwick, NSW 2031, Australia.

B School of Chemistry and Biological Resources Imaging Laboratory, University of New South Wales, High Street, Kensington, NSW 2052, Australia.

C Institute of Clinical Physiology, National Research Council (CNR), Via G. Moruzzi, Pisa 56124, Italy.

D Department of Pharmacy, University of Pisa, Via Bonanno Pisano, Pisa 56126, Italy.

E Corresponding author. Email: g.pascali@unsw.edu.au

Australian Journal of Chemistry 74(6) 443-452 https://doi.org/10.1071/CH20247
Submitted: 12 August 2020  Accepted: 21 December 2020   Published: 1 February 2021

Journal Compilation © CSIRO 2021 Open Access CC BY-NC-ND

Abstract

We successfully radiolabelled a novel prospective cannabinoid type 2 receptor ligand with 18F 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. SOD1G93A 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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