Heliyon (Jun 2021)

Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

  • Lisa A. Stott,
  • Cheryl A. Brighton,
  • Jason Brown,
  • Richard Mould,
  • Kirstie A. Bennett,
  • Robert Newman,
  • Heather Currinn,
  • Flavia Autore,
  • Alicia P. Higueruelo,
  • Benjamin G. Tehan,
  • Cliona MacSweeney,
  • Michael A. O'Brien,
  • Steve P. Watson

Journal volume & issue
Vol. 7, no. 6
p. e07201

Abstract

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The identification of cannabinoid ligands Cannabidiol and O-1918 as inverse agonists of the orphan receptor GPR52 is reported. Detailed characterisation of GPR52 pharmacology and modelling of the proposed receptor interaction is described. The identification of a novel and further CNS pharmacology for the polypharmacological agent and marketed drug Cannabidiol is noteworthy.

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