Kamei C, Mio M, Kitazumi K, Tsujimoto S, Yoshida T, Adachi Y, Tasaka K
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Japan.
Immunopharmacol Immunotoxicol. 1992;14(1-2):207-18. doi: 10.3109/08923979209009220.
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.
在大鼠、豚鼠和兔子身上测试了依巴斯汀的抗组胺和抗血小板活化因子（PAF）作用。依巴斯汀显示出强效的组胺H1阻断作用，但在组胺诱导的豚鼠回肠收缩和组胺诱导的大鼠皮肤反应中，其效力略低于酮替芬。在大鼠组胺诱导的染料渗漏到鼻腔的试验中，该药物比酮替芬和氮卓斯汀稍强。与特异性PAF拮抗剂WEB 2086相比，依巴斯汀以及酮替芬在较高浓度下可抑制PAF诱导的兔血小板聚集。在PAF诱导的豚鼠支气管痉挛中，依巴斯汀在抑制支气管收缩方面比酮替芬更有效，而对PAF诱导的低血压无明显作用。依巴斯汀对LTC4诱导的离体豚鼠气管收缩产生强效拮抗作用。总之，依巴斯汀强效的抗组胺、抗PAF和抗白三烯（LT）作用可能对其抗过敏活性有显著贡献。
