Leukotriene and Related Receptors

Supporting information

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.

To view external sources of pharmacological information for Leukotriene and Related Receptors, please click here: IUPHAR Receptor Code and BJP Guide

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
BLT1 Human LTB4R NM_181657 Q15722
Mouse Ltb4r1 NM_008519 O88855
Rat Ltb4r NM_021656 Q9R0Q2
BLT2 Human LTB4R2 NM_019839 Q9NPC1
Mouse Ltb4r2 NM_020490 Q9JJL9
Rat Ltb4r2 NM_053640 Q924U0
View all Leukotreine and Related Receptor Gene Data »

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