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Zafirlukast

产品号 DB00549 公司名称 DrugBank
CAS号 107753-78-6 公司网站 http://www.ualberta.ca/
分子式 C31H33N3O6S 电 话 (780) 492-3111
分子量 575.67522 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 431

产品价格信息

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产品别名

标题
Zafirlukast
IUPAC标准名
cyclopentyl N-[3-({2-methoxy-4-[(2-methylbenzenesulfonyl)carbamoyl]phenyl}methyl)-1-methyl-1H-indol-5-yl]carbamate
IUPAC传统名
cyclopentyl N-[3-({2-methoxy-4-[(2-methylbenzenesulfonyl)carbamoyl]phenyl}methyl)-1-methylindol-5-yl]carbamate
商标名
Accolate
别名
zafirlukast

产品登记号

PubChem CID 5717
CAS号 107753-78-6
PubChem SID 46506874

产品性质

疏水性(logP) 5.4

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved; investigational
Description Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), which is usually taken just once daily.

Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.
Indication For the prophylaxis and chronic treatment of asthma.
Pharmacology Zafirlukast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA) indicated for the prophylaxis and chronic treatment of asthma. Patients with asthma were found in one study to be 25-100 times more sensitive to the bronchoconstricting activity of inhaled LTD4 than nonasthmatic subjects. In vitro studies demonstrated that zafirlukast antagonized the contractile activity of three leukotrienes (LTC4, LTD4 and LTE4) in conducting airway smooth muscle from laboratory animals and humans. Zafirlukast prevented intradermal LTD4-induced increases in cutaneous vascular permeability and inhibited inhaled LTD4-induced influx of eosinophils into animal lungs.
Toxicity Side effects include rash and upset stomach.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic
Absorption Rapidly absorbed following oral administration, reduced following a high-fat or high-protein meal.
Half Life 10 hours
Protein Binding 99%
Elimination The most common metabolic products are hydroxylated metabolites which are excreted in the feces.
Distribution * 70 L
Clearance * apparent oral cl=20 L/h
* 11.4 L/h [7-11 yrs]
* 9.2 L/h [5-6 yrs]
External Links
Wikipedia
RxList
Drugs.com

参考文献