Product Name

Zafirlukast

CAS Number

107753-78-6

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Product Name:
Zafirlukast
CAS Number:
107753-78-6
Indication:
For the prophylaxis and chronic treatment of asthma.
Mode of Action:

Zafirlukast is a selective and competitive receptor antagonist of leukotriene D_ and E_ (LTD_ and LTE_), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.

Pharmacodynamics:

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.

Metabolism:

Hepatic

Toxicity:

Side effects include rash and upset stomach.

IUPAC:
cyclopentyl N-{3-[(2-methoxy-4-{[(2-methylbenzene)sulfonyl]carbamoyl}phenyl)methyl]-1-methyl-1H-indol-5-yl}carbamate
ATC:
R03DC01
PubChem:
5717
DrugBank:
DB00549 (APRD00377)
Formula:
C9H13N3O3
Molecular Mass:
575.675
SMILES:
COC1=C(CC2=CN(C)C3=C2C=C(NC(=O)OC2CCCC2)C=C3)C=CC(=C1)C(=O)NS(=O)(=O)C1=CC=CC=C1C
AHFS Code:
48:10.2
InChi:
YEEZWCHGZNKEEK-UHFFFAOYSA-N

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