Leukotriene and Related Receptors

Leukotriene and related receptors are activated by the endogenous ligands leukotriene (LT) B₄, LTC₄, LTD₄, LTE₄ and 12-HETE. Leukotrienes are lipid mediators synthesized from arachidonic acid by lipoxygenase enzymes. They act on peroxisome-proliferating receptors (PPARs) as well as the G-protein-coupled leukotriene receptors, and are important in inflammatory signaling pathways.

Leukotriene and related receptors are high affinity stereoselective receptors that have a wide biological distribution. BLT₁ and BLT₂ receptors are synthesized by polymorphonuclear leukocytes and are found at their highest concentrations on myeloid cells, mast cells and macrophages. CysLT₁ and CysLT₂ receptors are expressed most abundantly on myeloid cells. CysLT₂ has a suppressive effect on CysLT₁ expression, suggesting that it has an autoregulatory role on CysLT₁ levels.

The main role of CysLT receptors is contraction of vascular, respiratory and gastrointestinal smooth muscle. The lipoxin A₄ receptor (ALX) is expressed in high concentrations on neutrophils and has been suggested to mediate pro-inflammatory actions. The oxoeicosanoid receptor (OXE) is expressed in high concentrations on eosinophils, neutrophils and monocytes and is involved in chemotaxis and intracellular calcium mobilization.

External sources of pharmacological information for Leukotriene and Related Receptors :

• IUPHAR Receptor Code

• BJP Guide

Leukotriene and Related Receptor Gene Data