Chemical Tools for Studying Lipid-Binding Class A G Protein-Coupled Receptors

Pharmacol Rev. 2017 Jul;69(3):316-353. doi: 10.1124/pr.116.013243.


Cannabinoid, free fatty acid, lysophosphatidic acid, sphingosine 1-phosphate, prostanoid, leukotriene, bile acid, and platelet-activating factor receptor families are class A G protein-coupled receptors with endogenous lipid ligands. Pharmacological tools are crucial for studying these receptors and addressing the many unanswered questions surrounding expression of these receptors in normal and diseased tissues. An inherent challenge for developing tools for these lipid receptors is balancing the often lipophilic requirements of the receptor-binding pharmacophore with favorable physicochemical properties to optimize highly specific binding. In this study, we review the radioligands, fluorescent ligands, covalent ligands, and antibodies that have been used to study these lipid-binding receptors. For each tool type, the characteristics and design rationale along with in vitro and in vivo applications are detailed.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Humans
  • Ligands
  • Lipid Metabolism
  • Lipids / analysis*
  • Receptors, G-Protein-Coupled / analysis*
  • Receptors, G-Protein-Coupled / metabolism*


  • Ligands
  • Lipids
  • Receptors, G-Protein-Coupled