Effect of Y-24180, a platelet-activating factor-receptor antagonist, on the antigen-induced airway microvascular leakage in guinea pigs

Japanese Journal of Pharmacology
Y IwahisaM Terasawa

Abstract

The inhibitory effect of Y-24180 ((+/-)-4-(2-chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]-6, 9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) on platelet-activating factor (PAF)- or antigen-induced airway microvascular leakage was studied in guinea pigs by oral administration. The tissue content of extravasated Evans blue dye was used as an index of plasma exudation in the trachea, main bronchi, central intrapulmonary airways and peripheral intrapulmonary airways. In all of these tissues, Y-24180 potently inhibited the leakage induced by PAF. The ED50 value of Y-24180 determined in each of the tissues was approximately 0.02 mg/kg, demonstrating that the inhibitory potency of Y-24180 is 4-6 times that of WEB 2086, another PAF antagonist. Even at a dose of 10 mg/kg, however, Y-24180 showed no inhibitory effect on the leakage induced by leukotriene (LT) D4, histamine or bradykinin. In the antigen-induced model of guinea pigs sensitized with aerosolized ovalbumin, Y-24180 (0.1-10 mg/kg) and WEB 2086 (1-100 mg/kg) potently inhibited the microvascular leakage in all of the examined airway tissues except for the trachea. At 1-100 mg/kg, however, both ONO-1078, an LT-receptor antagonist, and OKY-046, a thromboxane A2 syn...Continue Reading

Citations

Jan 22, 2005·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Chung-Ren Jan, Yu-Ying Chao
Dec 9, 2003·Life Sciences·Yu-Ying Chao, Chung-Ren Jan

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