Montelukast (sodium salt)

Montelukast is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50 = 4.9 nM in HEK293 cell membranes expressing the human receptor).{14081} It is selective for CysLT1 over CysLT2 receptors (IC50 = >10,000 nM in COS-7 cell membranes expressing the human receptor).{8519} Montelukast inhibits bronchoconstriction induced by leukotriene D4 (LTD4; Item No. 20310) in anesthetized guinea pigs (ED50 = 69 nmol/kg, p.o.).{10911} It inhibits ovalbumin-induced airway hyperresponsiveness and increases in the number of total cells and eosinophils in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma when administered at doses of 3 and 10 mg/kg.{11231} Formulations containing montelukast have been used in the treatment of asthma, allergic rhinitis, and exercise-induced bronchoconstriction.