The enigmatic pharmacology of GPR55

Ruth Alexandra Ross

Research output: Contribution to journalLiterature reviewpeer-review

205 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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