Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.

Tipelukast inhibits the binding of [³H] LTD4 to the LTD4 receptors on pul-monary cell membrane of guinea-pigs (IC₅₀ = 2.3 μmol).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Fiftheen min after an aerosolized antigen challenge, and UNDW inhaled 5 min later into the guinea pigs, Tipelukast significantly alters the UNDW-induced bronchoconstriction. Tipelukast (1 and 5 mg/kg) administered intravenously 15 min after antigen challenge reduces the propranolol-induced bronchoconstriction (PIB) in a dose-dependent manner in guinea-pigs.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Fiftheen min after an aerosolized antigen challenge, and UNDW inhaled 5 min later into the guinea pigs, Tipelukast significantly alters the UNDW-induced bronchoconstriction. Tipelukast (1 and 5 mg/kg) administered intravenously 15 min after antigen challenge reduces the propranolol-induced bronchoconstriction (PIB) in a dose-dependent manner in guinea-pigs.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Fujimura M, et al. No involvement of lipid mediators in a guinea pig model of ultrasonically nebulized distilled water-induced bronchoconstriction. Prostaglandins Other Lipid Mediat. 2000 Jan;60(1-3):49-58.  [Content Brief]

  . Fujimura M, et al. Role of leukotrienes in post-allergic propranolol-induced bronchoconstriction in guinea-pigs. Clin Exp Allergy. 1997 Oct;27(10):1219-26.  [Content Brief]