International Union of Basic and Clinical Pharmacology. LXXXIV: leukotriene receptor nomenclature, distribution, and pathophysiological functions

Pharmacol Rev. 2011 Sep;63(3):539-84. doi: 10.1124/pr.110.004184.


The seven-transmembrane G protein-coupled receptors activated by leukotrienes are divided into two subclasses based on their ligand specificity for either leukotriene B(4) or the cysteinyl leukotrienes (LTC(4), LTD(4), and LTE(4)). These receptors have been designated BLT and CysLT receptors, respectively, and a subdivision into BLT(1) and BLT(2) receptors and CysLT(1) and CysLT(2) receptors has been established. However, recent findings have also indicated the existence of putative additional leukotriene receptor subtypes. Furthermore, other ligands interact with the leukotriene receptors. Finally, leukotrienes may also activate other receptor classes, such as purinergic receptors. The aim of this review is to provide an update on the pharmacology, expression patterns, and pathophysiological roles of the leukotriene receptors as well as the therapeutic developments in this area of research.

Publication types

  • Review

MeSH terms

  • Animals
  • Cysteine / agonists
  • Cysteine / antagonists & inhibitors
  • Cysteine / metabolism
  • Gene Expression Regulation*
  • Humans
  • International Agencies
  • Leukotriene Antagonists / therapeutic use
  • Leukotrienes / agonists
  • Leukotrienes / metabolism
  • Molecular Targeted Therapy
  • Organ Specificity
  • Receptors, Leukotriene / chemistry
  • Receptors, Leukotriene / classification*
  • Receptors, Leukotriene / genetics
  • Receptors, Leukotriene / metabolism
  • Signal Transduction / drug effects
  • Terminology as Topic


  • Leukotriene Antagonists
  • Leukotrienes
  • Receptors, Leukotriene
  • cysteinyl-leukotriene
  • Cysteine