Fujimura H, Tsurumi K, Yanagihara M, Hiramatsu Y, Tamura Y, Shimizu Y, Hojo M, Yoshida Y, Akimoto Y
Nihon Yakurigaku Zasshi. 1981 Oct;78(4):291-303. doi: 10.1254/fpj.78.291.
The anti-allergic effect of Mequitazine (LM-209) which was found to have an anti-histaminic activity was investigated in guinea-pigs. The inhibitory activities of LM-209 on the Schultz-Dale reaction and ileum contraction by some mediators released from the sensitized guinea-pig lung were the same as those of clemastine fumarate (CL) but with 5 times the potency. LM-209 and CL, but these activities were less potent than in the case of disodium cromoglycate. The various anaphylactic reactions mediated by IgG in guinea-pigs were inhibited by LM-209, CL and chlorpheniramine maleate (CPM). The homologous PCA mediated IgE in rats was also inhibited by LM-209, CL and CPM, but the duration of the action with LM-209 was markedly longer. In experimentally-induced asthma, the decrease of respiratory rate and volume was significantly inhibited by LM-209, but was not affected by CL. Thus, LM-209 seems to inhibit the allergic reaction mainly by an antagonistic action on allergic mediators.
已发现具有抗组胺活性的美喹他嗪（LM - 209）的抗过敏作用在豚鼠身上进行了研究。LM - 209对致敏豚鼠肺释放的某些介质引起的舒尔茨 - 戴尔反应和回肠收缩的抑制活性与富马酸氯马斯汀（CL）相同，但效力为其5倍。LM - 209和CL，但这些活性比色甘酸二钠的情况弱。豚鼠中由IgG介导的各种过敏反应被LM - 209、CL和马来酸氯苯那敏（CPM）抑制。大鼠中由IgE介导的同源被动皮肤过敏反应也被LM - 209、CL和CPM抑制，但LM - 209的作用持续时间明显更长。在实验性诱发的哮喘中，LM - 209显著抑制呼吸频率和容积的降低，但CL对此无影响。因此，LM - 209似乎主要通过对过敏介质的拮抗作用来抑制过敏反应。
