Emedastine difumarate 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,Ki值为 1.3 nM。Emedastine difumarate 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。
生物活性 | Emedastine difumarate is an orally active, selective and high affinityhistamineH1receptorantagonist with aKivalue of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3]. |
IC50& Target[1] | H1Receptor 1.3 nM (Ki) | H2Receptor 49067 nM (Ki) | H3Receptor 12430 nM (Ki) |
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体外研究 (In Vitro) | Emedastine difumarate inhibits histamine H2receptor (Ki=49067 nM) and histamine H3receptor (Ki=12430 nM)[1]. High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2]. Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].
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体内研究 (In Vivo) | Emedastine difumarate (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[3]. Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3]. Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2]. Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2].
Animal Model: | Male ICR mice 5-6 weeks of age[3] | Dosage: | 0.03, 0.1, 0.3 mg/kg | Administration: | Orally; 30 min before pruritogen injection | Result: | Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |