Preliminary Investigation of a Novel
| Autor: | Piero A. Salvadori, Valentina Lucchesi, Giuseppe Saccomanni, Giancarlo Pascali, Clementina Manera, Simone Zanoni, Elena Sanguinetti, Daniele Panetta, Silvia Burchielli, Mariarosaria De Simone, Patricia Iozzo |
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| Rok vydání: | 2021 |
| Předmět: |
Biodistribution
medicine.diagnostic_test Mesylate medicine.medical_treatment Radiochemistry General Chemistry Ligand (biochemistry) High-performance liquid chromatography 030218 nuclear medicine & medical imaging 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine chemistry Positron emission tomography Cannabinoid receptor type 2 medicine Cannabinoid Receptor 030217 neurology & neurosurgery |
| Zdroj: | Australian Journal of Chemistry. 74:443-452 |
| ISSN: | 1445-0038 0004-9425 |
| DOI: | 10.1071/ch20247 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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