Takahashi K, Endoh K, Yamada N, Kadowaki S, Arai Y, Sugasawa K
Nihon Yakurigaku Zasshi. 1986 Sep;88(3):245-54. doi: 10.1254/fpj.88.245.
The effects of a new anti-allergic agent, MY-5116: isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylate, on experimental animal models of type I approximately type IV allergic reactions and the formation of IgE antibody were investigated. MY-5116 administered intraperitoneally at doses of 30 and 100 mg/kg suppressed significantly the homologous PCA in guinea pigs. MY-5116 administered intraperitoneally at the dose of 100 mg/kg also suppressed significantly the heterologous PCA in guinea pigs. MY-1250, the main active metabolite of MY-5116, showed no suppression on the Schultz-Dale reaction in guinea pigs, and MY-5116 showed no inhibition on the active systemic anaphylaxis in mice (type I). MY-5116 showed no inhibition on the reversed cutaneous anaphylaxis in rats (type II), the Forssman reaction in guinea pigs (type II), the Arthus reaction in mice (type III) and the delayed type hypersensitivity in mice (type IV). MY-5116 showed no suppression on the formation of IgE antibody in C3H/He and BALB/c mice and rats. From these results, it is concluded that MY-5116 selectively suppresses the experimental models of type I allergic reaction.
新型抗过敏药物MY-5116（5,6-二氢-7,8-二甲基-4,5-二氧代-4H-吡喃并[3,2-c]喹啉-2-羧酸异戊酯）对I型至IV型过敏反应实验动物模型及IgE抗体形成的影响进行了研究。以30和100mg/kg的剂量腹腔注射MY-5116可显著抑制豚鼠的同种被动皮肤过敏反应（PCA）。以100mg/kg的剂量腹腔注射MY-5116也可显著抑制豚鼠的异种PCA。MY-5116的主要活性代谢产物MY-1250对豚鼠的舒尔茨-戴尔反应无抑制作用，MY-5116对小鼠的主动全身过敏反应（I型）无抑制作用。MY-5116对大鼠的反向皮肤过敏反应（II型）、豚鼠的福斯曼反应（II型）、小鼠的阿瑟斯反应（III型）和小鼠的迟发型超敏反应（IV型）均无抑制作用。MY-5116对C3H/He和BALB/c小鼠及大鼠中IgE抗体的形成无抑制作用。从这些结果可以得出结论，MY-5116选择性地抑制I型过敏反应的实验模型。
