The cysteinyl leukotrienes (CysLTs) LTC₄ and LTD₄ are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of G protein-coupled receptors, CysLT₁ and CysLT₂.^1,2,3 HAMI3379 is a potent cysteinyl leukotriene 2 (CysLT₂) receptor antagonist that inhibits radioligand binding of LTD₄ to CysLT₂ and CysLT₁ receptor cell lines with IC₅₀ values of 37.9 and >30,000 nM, respectively.⁴ In a CysLT₂ receptor reporter cell line, HAMI3379 antagonizes LTD₄– and LTC₄-induced intracellular calcium mobilization with IC₅₀ values of 3.8 and 4.4 nM, respectively, whereas it only weakly inhibits that for a CysLT₁ receptor reporter cell line (IC₅₀ = >10,000 nM).⁴ In isolated Langendorff-perfused guinea pig hearts, HAMI3379 reverses the LTC₄-stimulated increase in perfusion pressure and decrease in contractility.⁴

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1.Lynch, K.R.,O’Neill, G.P.,Liu, Q., et al. Characterization of the human cysteinyl leukotriene CysLT₁ receptor. Nature 399, 789-793 (1999).

2.Heise, C.E.,O’Dowd, B.F.,Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J. Biol. Chem. 275, 30531-30536 (2000).

3.Sarau, H.M.,Ames, R.S.,Chambers, J., et al. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Mol. Pharmacol. 56, 657-663 (1999).

4.Wunder, F.,Tinel, H.,Kast, R., et al. Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT₂) receptor. British Journal of Pharmacology 160, 399-409 (2010).