Abstract
We report the synthesis of terminally fluorinated HU-210 and HU-211 analogues (HU-210F and HU-211F, respectively) and their biological evaluation as ligands of cannabinoid receptors (CB1 and CB2) and N-methyl D-aspartate receptor (NMDAR). [18F]-labelled HU-210F was radiosynthesised from the bromo-substituted precursor. In vitro assays showed that both HU-210F and HU-211F retain the potent pharmacological profile of HU-210 and HU-211, suggesting that [18F]-radiolabelled HU-210F and HU-211F could have potential as PET tracers for in vivo imaging.
Original language | English |
---|---|
Pages (from-to) | 2086-2096 |
Number of pages | 11 |
Journal | Organic & Biomolecular Chemistry |
Volume | 15 |
Issue number | 9 |
Early online date | 10 Feb 2017 |
DOIs | |
Publication status | Published - 2017 |