1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE

Description

Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B₄ (LTB₄) have been potential drug development targets for several years. The tetrazole LY255283 is a competitive antagonist of the BLT₂ receptor. It displaces radiolabeled LTB₄ from guinea pig lung membrane, with an IC₅₀ of about 100 nM. LY255283 exhibits IC₅₀ values of ~950 nM and >10 μM at human recombinant BLT₂ and BLT₁ receptors, respectively. LY255283 inhibits eosinophil chemotaxis by 80% at a concentration of 10 μM, and inhibits the binding of radiolabeled LTB₄ to eosinophil membranes with an IC₅₀ of 260 nM.

Uses

LY-255283 is a selective, competitive BLT2 receptor antagonist used in the treatment of chronic myeloid leukemia.

Definition

ChEBI: 1-[5-ethyl-2-hydroxy-4-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenyl]ethanone is an aromatic ketone.

Biological Activity

Selective, competitive antagonist of BLT 2 receptors (IC 50 values are ~ 1 and > 10 μ M at human recombinant BLT 2 and BLT 1 receptors respectively). Inhibits LTB 4 -induced contraction of lung parenchyma (pA 2 = 7.2), and reduces LTB 4 -mediated airway obstruction in guinea pigs following i.v. and oral administration.

storage

Store at +4°C

References

[1] STEVEN A. SILBAUGH . Pulmonary actions of LY255283, a leukotriene B4 receptor antagonist[J]. European journal of pharmacology, 1992, 223 1: Pages 57-64. DOI: 10.1016/0014-2999(92)90818-o
[2] IVAN M. RICHARDS. Contribution of Leukotriene B4 to Airway Inflammation and the Effect of Antagonists[J]. Annals of the New York Academy of Sciences, 1991, 629 1: 274-287. DOI: 10.1111/j.1749-6632.1991.tb37983.x