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Emedastine

CAS No. : 87233-61-2

MCE 国际站：Emedastine

产品活性：Emedastine 是一种具有口服活性，选择性和高亲和力的组胺 H₁ 受体拮抗剂，K_i 值为 1.3 nM。Emedastine 是一种苯并咪唑衍生物，具有强大的抗过敏特性，可用于过敏性鼻炎，过敏性皮肤疾病和过敏性结膜炎。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: Emedastine inhibits histamine H₂ receptor (K_i=49067 nM) and histamine H₃ receptor (K_i=12430 nM).
High concentrations of Emedastine (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts.
Emedastine (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration.

In Vivo: Emedastine (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg.
Pretreatment with Emedastine (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B.
Emedastine (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs.
Emedastine inhibits histamine-induced contractions of isolated ileum (IC₅₀=6.1 nM).

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