Martel P R, Klicius J, Pinski J
Can J Physiol Pharmacol. 1978 Dec;56(6):1005-10. doi: 10.1139/y78-160.
Passive anaphylaxis induced in the rat hind paw and peritoneal cavity with rat serum containing immunoglobulin E antibody was inhibited by N-(2-oxo-3,5,7-cycloheptatrien-1-yl)-aminooxoacetic acid ethyl ester (AY-25,674). In contrast with disodium cromoglycate (DSCG), AY-25,674 was orally active. Otherwise, the activity profile of AY-25,674 was similar to that of DSCG. Peak activity occurred a short time after administration, large doses produced tachyphylaxis, and anaphylactic histamine release from mast cells was inhibited. AY-25,674 did not inhibit increased vascular permeability produced by nonreaginic antibody, compound 48/80, serotonin, or histamine. It is concluded that AY-25,674 produces its antiallergic effects by inhibiting mediator release from mast cells by a mechanism similar to that of DSCG.
用含有免疫球蛋白E抗体的大鼠血清在大鼠后爪和腹腔中诱导的被动过敏反应被N-(2-氧代-3,5,7-环庚三烯-1-基)-氨基氧代乙酸乙酯(AY-25,674)抑制。与色甘酸钠(DSCG)相比,AY-25,674具有口服活性。此外,AY-25,674的活性谱与DSCG相似。给药后短时间出现活性峰值,大剂量产生快速耐受性,并且抑制肥大细胞释放过敏反应性组胺。AY-25,674不抑制非反应素抗体、化合物48/80、5-羟色胺或组胺所产生的血管通透性增加。结论是AY-25,674通过与DSCG类似的机制抑制肥大细胞释放介质而产生其抗过敏作用。