Cayman Leukotriene B4 Ethanolamide

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 (K_i = 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.

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