The enigmatic pharmacology of GPR55

Ruth Alexandra Ross

Research output: Contribution to journalLiterature review

195 Citations (Scopus)

Abstract

Preliminary data presented at conferences and in the patent literature introduced the possibility the orphan receptor GPR55 might account for some of the well-documented non-CB1, non-CB2 effects reported for certain cannabinoid ligands. Several peer-reviewed publications have recently emerged in which the pharmacology of the cannabinoids at GPR55 has been probed in more depth. Despite this, the classification of GPR55 as a cannabinoid receptor remains a contentious issue. The weight of evidence points to GPR55 as a receptor that is activated by certain cannabinoid ligands and by the bioactive lipid L-alpha-lysophosphatidylinsoitol. It couples to G(12) proteins, activates RhoA and mobilizes intracellular Ca2+, possibly in an agonist- and tissue-dependant manner, thus displaying 'agonist functional selectivity'. Here, I review the recent literature in an effort to glean the key controversies and outstanding questions surrounding the interaction between cannabinoids and this orphan receptor.

Original languageEnglish
Pages (from-to)156-163
Number of pages8
JournalTrends in Pharmacological Sciences
Volume30
Issue number3
Early online date21 Feb 2009
DOIs
Publication statusPublished - Mar 2009

Keywords

  • CANNABINOID RECEPTOR
  • ENDOGENOUS CANNABINOIDS
  • FUNCTIONAL SELECTIVITY
  • IDENTIFICATION
  • BRAIN
  • ANANDAMIDE
  • SYSTEM
  • CELLS
  • PAIN
  • CB2

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