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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.
Zanato, Chiara; Pelagalli, Alessia; Marwick, Katie F M; Piras, Monica; Dall'Angelo, Sergio; Spinaci, Andrea; Pertwee, Roger G; Wyllie, David J A; Hardingham, Giles E; Zanda, Matteo.
Afiliação
  • Zanato C; Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
  • Pelagalli A; Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
  • Marwick KF; Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, Scotland, UK.
  • Piras M; Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
  • Dall'Angelo S; Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
  • Spinaci A; Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
  • Pertwee RG; Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, Scotland, UK. m.zanda@abdn.ac.uk.
  • Wyllie DJ; Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, Scotland, UK.
  • Hardingham GE; Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, Scotland, UK.
  • Zanda M; 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.
Org Biomol Chem ; 15(9): 2086-2096, 2017 Mar 01.
Article em En | MEDLINE | ID: mdl-28210722
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.

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Org Biomol Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Org Biomol Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Reino Unido