Ishii H, Sasaki Y, Ikemura T, Kitamura S, Ohmori K
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.
Nihon Yakurigaku Zasshi. 1995 Oct;106(4):289-98. doi: 10.1254/fpj.106.289.
The present experiment was carried out to elucidate the antiallergic properties of KW-4679. Oral administration of KW-4679 showed a dose-dependent inhibition on the IgE-mediated 48-hr homologous PCA in rats, with an ID50 value of 0.04 mg/kg. Passive anaphylactic broncho-constriction in guinea pigs mediated by IgE-like homologous antibody against ovalbumin was prevented dose-dependently by treatment with KW-4679 at doses of 0.03-1 mg/kg, p.o. KW-4679 also inhibited the IgE-mediated active anaphylactic bronchoconstriction in rats. In passively sensitized guinea pigs, the inhalation of aerosol antigen decreased the dynamic compliance of the lung and increased the mean pulmonary resistance. Pretreatment with KW-4679 (0.03-1 mg/kg, p.o.) inhibited antigen-induced airway obstructions. Oral administration of KW-4679 significantly protected rats from compound 48/80-induced lethality. These results indicate that KW-4679 might be useful in the treatment of allergic diseases such as asthma.
进行本实验以阐明KW - 4679的抗过敏特性。口服KW - 4679对大鼠IgE介导的48小时同源被动皮肤过敏反应（PCA）呈现剂量依赖性抑制，半数抑制剂量（ID50）值为0.04 mg/kg。在豚鼠中，针对卵清蛋白的IgE样同源抗体介导的被动过敏性支气管收缩，经口服0.03 - 1 mg/kg剂量的KW - 4679可剂量依赖性地得到预防。KW - 4679还可抑制大鼠中IgE介导的主动过敏性支气管收缩。在被动致敏的豚鼠中，吸入气溶胶抗原会降低肺的动态顺应性并增加平均肺阻力。用KW - 4679（0.03 - 1 mg/kg，口服）预处理可抑制抗原诱导的气道阻塞。口服KW - 4679可显著保护大鼠免受化合物48/80诱导的致死作用。这些结果表明KW - 4679可能对治疗哮喘等过敏性疾病有用。
