Catalog No.S4211 Synonyms: MK-0476
Molecular Weight(MW): 608.17
Montelukast selectively antagonizes leukotriene D 4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1.
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|Description||Montelukast selectively antagonizes leukotriene D 4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1.|
Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. 
|In vivo||Montelukast (6 mg/kg, once per day for 20 d) significantly suppresses the increased eosinophils in BAL fluid and lung tissue, and increases IL-5 level in BAL fluid in OVA challenged mice. OVA challenge increases CysLT1 but decreases CysLT2 receptor mRNA expression. Montelukast inhibits the increased CysLT1 but not the reduces CysLT2 expression after OVA challenge. |
|In vitro||DMSO||100 mg/mL (164.42 mM)|
|Water||100 mg/mL (164.42 mM)|
|Ethanol||100 mg/mL (164.42 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01852812||Completed||Perennial Allergic Rhinitis||Merck Sharp & Dohme Corp.||June 7 2013||Phase 3|
|NCT01673620||Completed||Allergic Rhinitis||Merck Sharp & Dohme Corp.||July 4 2012||Phase 3|
|NCT02410278||Completed||Multiple Sclerosis||Biogen||June 29 2015||Phase 4|
|NCT00295022||Completed||Rhinitis Allergic Seasonal||UCB S.A. - Pharma Sector|UCB Pharma||July 29 2006||Phase 4|
|NCT00446056||Completed||Asthma||Merck Sharp & Dohme Corp.||September 25 2003||Phase 4|
|NCT02322671||Completed||Respiratory Disorders||GlaxoSmithKline||February 23 2015||Phase 1|
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