Biological Activity
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 Aβ1-42-induced CysLT1R expression and also suppresses Aβ1-42-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 Aβ1-42-induced memory impairment in mice, but has little effect on normal mice[4].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.