The effects of Leukotriene B4 (LTB4) are mediated by two known receptors, BLT1 and BLT2.1,2 LTB4 is a high affinity ligand for BLT1, and many of its pro-inflammatory effects are believed to be transduced through this receptor. The BLT2 is more enigmatic, in that LTB4 is not a high-affinity ligand, nor is it clear that BLT2 activation promotes inflammation. LTB4 ethanolamide (LTB4-EA) is a theoretical 5-LO metabolite of arachidonoyl ethanolamide (AEA). In CHO cells transfected with human BLTR1, LTB4-EA was a potent antagonist with about three times greater affinity for the receptor than LTB4 (Ki = 1.22 nM versus 3.88 nM). LTB4-EA antagonizes the LTB4-induced contractions of guinea pig lung parenchyma with an EC50 of 10 nM.3 LTB4-EA thus represents a potential endogenous anti-inflammatory compound functioning as a natural antagonist of BLTR1.
1
Yokomizo, T., Izumi, T., Chang, K., et al. A G-protein-coupled receptor for leukotriene B4 that mediates chemotaxis. Nature387620-624(1997).
2
Yokomizo, T., Kato, K., Terawaki, K., et al. A second leukotriene B4 receptor, BLT2: A new therapeutic target in inflammation and immunological disorders. J Exp Med193421-431(2000).
3
McHugh, D., McMaster, S., and Ross, R. Pharmacological characterization of LTB4 ethanolamide: Interaction with leukotriene (BLT) and vanilloid (TRPV1) receptors. 121(2003).
Yokomizo, T., Izumi, T., Chang, K., et al. A G-protein-coupled receptor for leukotriene B4 that mediates chemotaxis. Nature387620-624(1997).
Yokomizo, T., Kato, K., Terawaki, K., et al. A second leukotriene B4 receptor, BLT2: A new therapeutic target in inflammation and immunological disorders. J Exp Med193421-431(2000).
McHugh, D., McMaster, S., and Ross, R. Pharmacological characterization of LTB4 ethanolamide: Interaction with leukotriene (BLT) and vanilloid (TRPV1) receptors. 121(2003).
Leukotriene B4 Ethanolamide is available in the following screening
library: