LY255283 is selective, competitive antagonist of BLT2 receptors (IC50 values are ~ 1 and > 10 μM at human recombinant BLT2 and BLT1 receptors respectively), and inhibits LTB4-induced contraction of lung parenchyma (pA2 = 7.2), and reduces LTB4-mediated airway obstruction in guinea pigs following i.v. and oral administration.
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LY255283 is an antagonist to the LTB4 receptor (BLT2), demonstrating an IC50 of approximately 100 nM for blocking [3H]LTB4 binding in guinea pig lung membranes[1].[2].[3].[4].
体内研究
In pig models, LY255283 administered at doses of 3 and 30 mg/kg significantly alleviates lipopolysaccharide-induced acute respiratory distress syndrome (ARDS), likely through inhibiting the infiltration of activated polymorphonuclear neutrophils (PMNs) into the alveoli in a dose-responsive manner[3].
Furthermore, at a dosage of 2.5 mg/kg (intraperitoneally), it hinders the metastasis of transitional cell carcinoma in mouse models, indicating the critical involvement of a BLT2–Nox–ROS–NF–κB pathway in bladder cancer invasion and metastasis[4].
体外研究
LY255283 effectively competes with LTB4, diminishing contractile responses in lung parenchyma (pA2 = 7.2)[2].
Administered at a concentration of 10 μM for 7 days, LY255283 notably reduces the invasiveness of 253 J-BV bladder cancer cells, which are known for their high aggressiveness[4].
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