Maruyama Y, Terasawa M, Goto K, Oe T
Nihon Yakurigaku Zasshi. 1978 Mar;74(2):179-91. doi: 10.1254/fpj.74.179.
The IgE mediated reactions such as 48 hr homologous passive cutaneous anaphylaxis (PCA) and active anaphylactic bronchoconstriction in rats were inhibited in a dose dependent manner by treatment with 7-acetyl-5-oxo-5H-[1]benzopyranol[2,3-b] pyridine (Y-9000) and disodium cromoglycate (DSCG) given intraperitoneally. The inhibitory activity of Y-9000 was to the same extent as that seen with DSCG. The IgE mediated reactions were also inhibited by oral treatment with Y-9000 but not with DSCG. In addition, the treatment with Y-9000 resulted in inhibition of IgG mediated reaction such as anaphylactic asthma in the passively sensitized guinea pigs and 4 hr heterologous PCA in rats. However, DSCG failed to prevent these reactions. Y-9000 also inhibited the active systemic anaphylaxis of the mouse and non-immunological reactions in rats such as histamine release after an intraperitoneal injection of dextran, anaphylactoid reaction and paw edema induced by the dextran, egg white or carrageenin. This agent had a stimulating effect on the adrenals, and showed glucocorticoid like activity, but bronchodilator and antagonistic activities on chemical mediators were nil. These results suggest that the anti-allergic activities of Y-9000 are elicited by inhibiting the release of allergic mediators in a manner similar to DSCG, and are partially mediated by stressor activity.
腹腔注射7-乙酰-5-氧代-5H-[1]苯并吡喃并[2,3-b]吡啶(Y-9000)和色甘酸二钠(DSCG)可剂量依赖性抑制大鼠体内IgE介导的反应,如48小时同源被动皮肤过敏反应(PCA)和主动过敏性支气管收缩。Y-9000的抑制活性与DSCG相当。口服Y-9000也可抑制IgE介导的反应,但口服DSCG则无此作用。此外,Y-9000治疗可抑制IgG介导的反应,如被动致敏豚鼠的过敏性哮喘和大鼠4小时异源PCA。然而,DSCG无法预防这些反应。Y-9000还可抑制小鼠的主动全身过敏反应以及大鼠的非免疫反应,如腹腔注射右旋糖酐后的组胺释放、右旋糖酐、蛋清或角叉菜胶诱导的类过敏反应和爪肿胀。该药物对肾上腺有刺激作用,表现出糖皮质激素样活性,但对化学介质无支气管扩张和拮抗活性。这些结果表明,Y-9000的抗过敏活性是通过与DSCG类似的方式抑制过敏介质释放而产生的,并且部分由应激活性介导。