ANTIALLERGIC EFFECT OF EPINASTINE (WAL-801-CL) ON IMMEDIATE HYPERSENSITIVITY REACTIONS .2. ANTAGONISTIC EFFECT OF EPINASTINE ON CHEMICAL MEDIATORS, MAINLY ANTIHISTAMINIC AND ANTI-PAF EFFECTS

被引:19
作者
KAMEI, C [1 ]
MIO, M [1 ]
KITAZUMI, K [1 ]
TSUJIMOTO, S [1 ]
YOSHIDA, T [1 ]
ADACHI, Y [1 ]
TASAKA, K [1 ]
机构
[1] OKAYAMA UNIV,FAC PHARMACEUT SCI,DEPT PHARMACOL,OKAYAMA 700,JAPAN
关键词
D O I
10.3109/08923979209009220
中图分类号
R392 [医学免疫学]; Q939.91 [免疫学];
学科分类号
100102 ;
摘要
Anti-histamine and anti-PAF effects of epinastine were tested in rats, guinea pigs and rabbits. Epinastine showed a potent histamine H1-blocking effect, but the potency was slightly less than that of ketotifen in histamine-induced contraction of guinea pig ileum and histamine-induced cutaneous reactions in rats. In histamine-induced dye leakage into the nasal cavity tested in rats, the drug was slightly more potent than ketotifen and azelastine. Epinastine as well as ketotifen suppressed rabbit platelet aggregation induced by PAF at higher concentrations compared with WEB 2086, a specific PAF-antagonist. In the bronchospasm induced by PAF in guinea pigs, epinastine was more effective than ketotifen in inhibiting the bronchoconstriction, while it showed no remarkable effect on the hypotension induced by PAF. Epinastine caused a potent antagonistic effect on LTC4-induced contraction of isolated guinea pig trachea. In conclusion, the potent anti-histamine, anti-PAF and anti-LT effects of epinastine may significantly contribute to its antiallergic activity.
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页码:207 / 218
页数:12
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