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Synthesis, radio-synthesis and in vitro evaluation of terminally fluorinated derivatives of HU-210 and HU-211 as novel candidate PET tracers.
Organic & Biomolecular Chemistry 2017 March 2
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). [18 F]-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 [18 F]-radiolabelled HU-210F and HU-211F could have potential as PET tracers for in vivo imaging.
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