LTD4 antagonist 1 is a potent, orally active antagonist of leukotriene D4 (LTD4) with a Ki of 0.57 nM.
LTD4 antagonist 1 (Compound 38b) exhibits a Ki of 0.57 nM for displacement of [3H]LTD4 on guinea pig lung membranes, a pKB of 9.93±0.14 versus LTE4 on guinea pig trachea[1].
LTD4 antagonist 1 (Compound 38b) exhibits a po ED50/iv ED50 of 1.44 and 0.036 μmol/kg in LTD4-induced bronchoconstriction in guinea pigs[1].
[1]. Robert T. Jacobs, et al. Synthesis, Structure-Activity Relationships, and Pharmacological Evaluation of a Series of Fluorinated 3-Benzyl-5-Indolecarboxamides: Identification of 4-[[5-[((2R)-2-Methyl-4,4,4-trifluorobutyl)carbamoyl]-1-methylindol-3-yl]methyl]-3methoxy-N-[(2-methylphenyl)sulfonyl]benzamide, a Potent, Orally Active Antagonist of Leukotrienes D4 and E4. Journal of Medicinal Chemistry (1994), 37(9), 1282-97.