Emedastine 是一种可口服的，选择性和高亲和力的组胺H1受体拮抗剂，Ki值为 1.3 nM。它是苯并咪唑衍生物，可用于过敏性鼻炎、过敏性皮肤疾病和过敏性结膜炎的研究。

Emedastine is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

87233-61-2

C17H26N4O

302.422

LY188695;依美斯汀;Emadine;Emedastine

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years