Montelukast is a potent, selective and orally-active antagonist of the cysteinyl leukotriene 1 (CysLT1) receptor, with an IC50 value of 4.9 nM in HEK293 cell membranes expressing human CysLT1 receptors. The CysLT1 receptor is a receptor for cysteinyl leukotrienes (e.g. LTC4, LTD4, and LTE4) which mediate allergic and hypersensitivity reactions in a variety of inflammatory disorders, in particular asthma. Montelukast has been introduced clinically for the treatment of asthma, allergic rhinitis, and exercise-induced bronchoconstriction.
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