Kuriki H, Saijo T, Maki Y, Kanno M
Jpn J Pharmacol. 1979 Jun;29(3):385-97. doi: 10.1254/jjp.29.385.
A newly synthesized compound, 6-ethyl-3-(1H-tetrazol-5-yl)chromone (AA-344) given intravenously or orally inhibited considerably the 72-hr passive cutaneous anaphylaxis (72-hr PCA) induced by IgE in rats. The antiallergic action of AA-344 was neither due to the antihistamine or antiserotonin effect nor was it mediated via adrenergic mechanisms. The results obtained in a double sensitization with two IgE antibodies suggest that AA-344 may not impair antigen-antibody combination but probably prevents the release of chemical mediators including histamine. This assumption was supported by observation that AA-344 inhibited a reduction in the skin histamine content caused by the 72-hr PCA, without effect on the compound 48/80-induced histamine reduction. AA-344 also partially inhibited the IgGa-mediated 3-hr PCA in rats. These results indicate that the inhibitory action of AA-344 on the immediate hypersensitivity reactions is due to prevention of the release of chemical mediators from the mast cells, by acting on some process in sequential events leading to the mediator release following antigen-antibody combination.
一种新合成的化合物,6-乙基-3-(1H-四氮唑-5-基)色酮(AA-344),静脉注射或口服给药时,能显著抑制大鼠中由IgE诱导的72小时被动皮肤过敏反应(72小时PCA)。AA-344的抗过敏作用既不是由于抗组胺或抗血清素作用,也不是通过肾上腺素能机制介导的。用两种IgE抗体进行双重致敏所获得的结果表明,AA-344可能不会损害抗原-抗体结合,但可能会阻止包括组胺在内的化学介质的释放。这一假设得到了以下观察结果的支持:AA-344抑制了72小时PCA引起的皮肤组胺含量的降低,而对化合物48/80诱导的组胺降低没有影响。AA-344还部分抑制了大鼠中IgGa介导的3小时PCA。这些结果表明,AA-344对速发型超敏反应的抑制作用是由于通过作用于抗原-抗体结合后导致介质释放的一系列事件中的某个过程,从而防止肥大细胞释放化学介质。