MrgprX2-IN-2(Compound example 12)是一种专一的 Mas 相关 G 蛋白偶联受体 X2 (MRGPRX2) 拮抗剂。它通过抑制 MRGPRX2 引发的肥大细胞脱颗粒和炎症介质释放,阻断非IgE依赖的免疫反应。MrgprX2-IN-2 可用于假性过敏反应、慢性瘙痒症及炎症性疾病的研究。
Mizolastine dihydrochloride is a histamine H1-receptor antagonist (IC50: 47 nM). It also used in the treatment of hay fever, hives, and other allergic reactions.
EP6 is an inhibitor of 5-lipoxygenase (5-LO), which is a crucial enzyme of the arachidonic acid (AA) cascade and catalyzes the formation of bioactive leukotrienes (LTs) which are involved in inflammatory diseases and allergic reactions.
Tylogenin, a steroidal aglycone generated by acid hydrolysis from two seasonal glycosides occurring in Tylophora sylvatica, inhibits IgE-induced basophil mediator release for allergic reactions. In the rabbit basophil-dependent serotonin release (BDSR) assay system, the inhibitory activity of tylogenin was significantly greater than that of its parent glycosides, tylophoroside and acetyltylophoroside, and that of dexamethasone. The activity of tylogenin was found to increase with the incubation time. In the human leukocyte-dependent histamine release test model, the glycosides had only a minimal activity. In contrast, tylogenin, with a geom mean IC50 = 49 microM, exerted a significantly greater potency than dexamethasone. These results suggest that tylogenin could represent a new class of antiallergic agents.