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药品详细

Cinalukast(西那司特)

化学结构式图
中文名
西那司特
英文名
Cinalukast
分子式
C23H28N2O3S
化学名
3-({3-[(E)-2-(4-cyclobutyl-1,3-thiazol-2-yl)ethenyl]phenyl}carbamoyl)-2,2-diethylpropanoic acid
分子量
Average: 412.545
Monoisotopic: 412.182063462
CAS号
128312-51-6
ATC分类
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Used in the treatment of asthma, cinalukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Cinalukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phenylpropenes
    • Acetanilides
    Substructures
    • Carbonyl Compounds
    • Hydroxy Compounds
    • Alkanes and Alkenes
    • Acetates
    • Amino Ketones
    • Phenylpropenes
    • Benzene and Derivatives
    • Acetanilides
    • Carboxylic Acids and Derivatives
    • Cyclobutane and Derivatives
    • Thiazoles
    • Heterocyclic compounds
    • Aromatic compounds
    • Carboxamides and Derivatives
    • Imines
    • Keto-Acids
    • Styrene Derivatives
    • Anilines
    适应症
    药理
    Indication For Protection against second- phase inflamation in exercise-induced bronchoconstriction and Asthma.
    Pharmacodynamics Used in the treatment of asthma, cinalukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Cinalukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.
    Mechanism of action Binds to the cysteinyl leukotriene receptor. The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene receptors (CysLT) found in the human airway. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    logP 4 Not Available
    Predicted Properties
    Property Value Source
    water solubility 8.72e-04 g/l ALOGPS
    logP 4.98 ALOGPS
    logP 5.48 ChemAxon
    logS -5.7 ALOGPS
    pKa (strongest acidic) 4.36 ChemAxon
    pKa (strongest basic) 2.44 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 79.29 ChemAxon
    rotatable bond count 9 ChemAxon
    refractivity 116.75 ChemAxon
    polarizability 45.8 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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