Montelukast sodium 是可口服的半胱氨酸白三烯受体1 选择性拮抗剂，可用于研究预防哮喘和肝损伤。它还可减少心脏损伤，在肠缺血-再灌注损伤中也具有抗氧化作用。

Montelukast is an orally available leukotriene receptor antagonist which is widely used for the prophylaxis and chronic treatment of asthma and has been linked to rare cases of clinically apparent liver injury.

每天一次6 mg/kg Montelukast,服用20天后,明显抑制OVA激发的小鼠体内BAL液和肺组织中增多的嗜酸细胞,并且增加BAL液中IL-5水平. OVA激发会增加CysLT1S受体但会减少CysLT2受体的mRNA表达.OVA激发后,Montelukast抑制增加的CysLT1但不降低CysLT2的表达.

Montelukast通过与肺部和支气管中半胱氨酰白三烯受体CysLT1结合而阻断白三烯D4的作用,防止气道水肿,平滑肌收缩和分泌液粘稠,减少了由白三烯引起的支气管收缩,并减少炎症发生。

Nasal mucosa and polyp epithelial cells are stimulated with fetal bovine serum (FBS) with or without MK for 24 hours, and cytokine concentrations in epithelial secretions are measured by ELISA. After incubating peripheral blood eosinophils with epithelial cell-conditioned media (ECM) with or without montelukast up to 3 days, eosinophil survival is assessed by Trypan blue dye exclusion[1].

151767-02-1

C35H35ClNNaO3S

608.17

MK0476;孟鲁司特钠

H2O:30.4 mg/mL (50 mM)
DMSO:60.8 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years