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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.1 LY255283 exhibits IC50 values of ~950 nM and >10 µM at human recombinant BLT2 and BLT1 receptors, respectively.2 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.3
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1. Pulmonary actions of LY255283, a leukotriene B4 receptor antagonist. Eur. J. Pharmacol. 223, 57-64 (1992).
2. Hydroxyeicosanoids bind to and activate the low affinity leukotriene B4 receptor, BLT2. The Journal of Biological Chemisty 276(15), 12454-12459 (2001).
3. Contribution of leukotriene B4 to airway inflammation and the effect of antagonists. Ann. N. Y. Acad. Sci. 629, 274-287 (1991).