tcsc0548 Montelukast (sodium)

Montelukast (sodium) is a potent, selective CysLT₁ receptor antagonist.

In Vitro: Montelukast may contribute to the reduction of eosinophilic inflammation in upper-airway inflammatory diseases such as rhinitis and nasal polyposis. Montelukast has a significant inhibitory effect on FBS-induced GM-CSF, IL-6, and IL-8 secretion, but not sICAM-1, in nasal mucosa and polyp epithelial cells. Montelukast also shows an inhibitory effect (p<0.05) on ECM-induced eosinophil survival from both nasal mucosa and polyp epithelial cells^[1].

In Vivo: Montelukast significantly reduces mild, moderate, and part of severe exacerbations in chronic mild to moderate asthma, but it has inferior efficacy to ICS or ICS plus LABA^[2]. Rats with induced asthma have up-regulated NK1R expression in the airway, and montelukast can down regulate NK1R expression during airway remodeling^[3]. Blockade of CysLT₁R by repeated treatment with montelukast (1 or 2 mg/kg, ig, 4 weeks) reduces Aβ_1-42-induced CysLT₁R expression and also suppresses Aβ_1-42-induced increments of NF-κB p65, TNF-α, IL-1β and caspase-3 activation, and Bcl-2 downregulation in the hippocampus and cortex. Correspondingly, montelukast treatment significantly improves Aβ_1-42-induced memory impairment in mice, but has little effect on normal mice^[4].