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Powder: | Yes |
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Product Name | Montelukast Sodium |
Apperance | White to brownish |
CAS | 151767-02-1 |
MF | C35H37ClNNaO3S |
MW | 610.18 |
Pharmacological effect
Cysteinyl leukotrienes (LTC4, LTD4, LTE4) are eicanes with strong inflammatory effects released by various cells including mast cells and eosinophils. These important pre-asthma inflammatory mediators can bind to the cysteinyl leukotriene receptor (CysLT) found in the human airway, leading to various airway reactions. Including bronchial constriction, mucus secretion, increased vascular permeability and eosinophil aggregation.
Montelukast is a selective leukotriene receptor antagonist and has been approved for oral treatment of asthma and allergic rhinitis. It is also a powerful oral preparation that can significantly improve pro-inflammatory indicators. Biochemical and pharmacological bioassay showed that montelukast sodium had a high affinity and selectivity for the CysLT1 receptor (compared with other airway receptors of pharmacological significance such as prostaglandins, cholinergic and β -adrenergic receptors). Montelukast efficiently inhibits the physiological effects produced by the binding of LTCChemicalbook4, LTD4 and LTE4 to the CysLT1 receptor without any receptor agonizing activity. The second type of cysteinyl leukotriene receptor (CysLT2) exists in the lungs, but it may be confined to the blood vessels. So far, these two receptors have not been cloned. Therefore, the situation of the CysLT receptor is mainly described through receptor binding tests and pharmacological analyses. It is now believed that montelukast sodium does not antagonize the CysLT2 receptor.
Synthesis method
montelukast sodium is a selective oral leukotriene receptor antagonist developed by Merck of the United States and launched on the market in 1998. It can specifically inhibit cysteine leukotriene receptors. It is applicable to the prevention and long-term treatment of asthma in both adults and children, including the prevention of asthma symptoms during the day and night, the treatment of asthma patients sensitive to aspirin, and the prevention of bronchoconstriction caused by exercise.