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.
Zanato, C., Pelagalli, A., Marwick, K. F. M., Piras, M., Dall'Angelo, S., Spinaci, A., Pertwee, R. G., Wyllie, D. J. A., Hardingham, G. E., & Zanda, M. (2017). 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, 15(9), 2086-2096. https://doi.org/10.1039/C6OB02796B