ltd4 antagonist 1

LTD4 antagonist 1 is a potent and orally active antagonist of leukotriene D4 (LTD4; Ki: 0.57 nM).

LTD4 antagonist 2 (compound 6) functions as a leukotriene D4 (LTD4) antagonist with an IC50 of 2.8 μM for the cysteinyl leukotriene 1 receptor (CysLT1R). Additionally, it acts as an agonist for the G protein-coupled bile acid receptor 1 (GPBAR1), making it applicable for research into colitis, metabolic syndrome, and other GPBAR1- and CysLT1R-related diseases.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

Ritolukast (Wy-48252), an orally active aerosol leukotriene (LTD 4/E 4) receptor antagonist, effectively inhibits bronchoconstriction induced by aerosol LTD 4 in guinea pigs, demonstrating an ID 50 of 0.5mg/kg [1].