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 are important in inflammatory signaling pathways.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
2307 Leukotriene B4
BLT1/BLT2 receptor agonist and potent chemotactic factor

Antagonists

Cat No Product Name / Activity
3138 BAY-u 9773
Dual CysLT1 and CysLT2 antagonist
2025 Cinalukast
Potent, selective CysLT1 (LTD4) antagonist; orally active
2276 FPL 55712
Leukotriene receptor antagonist
2208 LY 255283
Selective, competitive BLT2 receptor antagonist
2338 MK 571
Potent CysLT1 (LTD4) inverse agonist. Also MRP1 inhibitor
5904 Montelukast sodium
CysLT1 and GPR17 antagonist
3026 ONO 1078
Selective CysLT1 antagonist
1804 SR 2640 hydrochloride
Potent, selective LTD4 /LTE4 receptor antagonist

Inhibitors

Cat No Product Name / Activity
4742 Gue 1654
Selective inhibitor of OXE-R Gβγ signaling

Other

Cat No Product Name / Activity
2756 Arachidonic acid (in Tocrisolve™100)
Endogenous free fatty acid (in water-soluble emulsion)
3541 BAY-X 1005
Orally active 5-lipoxygenase activating protein (FLAP) inhibitor
2709 Cilastatin sodium
Dipeptidase inhibitor; inhibits metabolism of LTD4 to LTE4
5979 Eicosapentaenoic Acid
Endogenous polyunsaturated fatty acid; inhibits leukotriene B4 synthesis
1311 MK 886
Inhibitor of 5-lipoxygenase-activating protein (FLAP)
0607 17-ODYA
LTB ω-hydroxylase inhibitor

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 :

Literature for Leukotriene and Related Receptors

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Leukotriene and Related Receptor Gene Data

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
CysLT1 Human CYSLTR1 NM_006639 Q9Y271
Mouse Cysltr1 NM_021476 Q99JA4
Rat Cysltr1 NM_053641 Q924T8
CysLT2 Human CYSLTR2 NM_020377 Q9NS75
Mouse Cysltr2 NM_133720 Q920A1
Rat Cysltr2 NM_133413 Q924T9
ALX Human FPR2 NM_001005738 P25090
Mouse Fpr3 NM_008042 O08790
OXE Human OXER1 NM_148962 Q8TDS5