Montelukast inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.
Montelukast causes inhibition of airway cysteinyl leukotriene receptors as demonstrated by the ability to inhibit bronchoconstriction due to inhaled LTD4 in asthmatics.
MK-0476, an LTD4
receptor antagonist, improves the signs and symptoms of asthma with a dose as low as 10mg once daily [abstract].
The latter, also known as leukotrienes (LTB4, LTC4, LTD4
, and LTE4), play an important role in attracting inflammatory cells to the airway, airway narrowing, and mucous secretion, all of which can induce asthma symptoms and potentially long-term lung damage.
Cysteinyl leukotrienes (LTC4, LTD4
, and LTE4) play a major role in broncho-constriction, mucus production, airway edema, and inflammation, all factors that contribute to asthma symptoms.