title: Synthesis, radio-synthesis and in vitro evaluation of terminally fluorinated derivatives of HU-210 and HU-211 as novel candidate PET tracers.
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 (CB1and 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.
authors.affiliation: Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
authors.forename: Chiara
authors.initials: C
authors.lastname: Zanato
authors.affiliation: Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
authors.forename: Alessia
authors.initials: A
authors.lastname: Pelagalli
authors.affiliation: Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, Scotland, UK.
authors.forename: Katie F M
authors.initials: KF
authors.lastname: Marwick
authors.affiliation: Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
authors.forename: Monica
authors.initials: M
authors.lastname: Piras
authors.affiliation: Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
authors.forename: Sergio
authors.initials: S
authors.lastname: Dall'Angelo
authors.affiliation: Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
authors.forename: Andrea
authors.identifier: http://orcid.org/0000-0002-5172-651X
authors.initials: A
authors.lastname: Spinaci
authors.affiliation: Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
authors.forename: Roger G
authors.identifier: http://orcid.org/0000-0003-3227-2783
authors.initials: RG
authors.lastname: Pertwee
authors.affiliation: Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, Scotland, UK.
authors.forename: David J A
authors.initials: DJ
authors.lastname: Wyllie
authors.affiliation: Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, Scotland, UK.
authors.forename: Giles E
authors.initials: GE
authors.lastname: Hardingham
authors.affiliation: Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk and C.N.R. - I.C.R.M., via Mancinelli 7, 20131 Milan, Italy.
authors.forename: Matteo
authors.identifier: http://orcid.org/0000-0002-8257-5232
authors.initials: M
authors.lastname: Zanda