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编 号：F490631
分子式：C25H34N4O9
分子量：534.56
分子式：C25H34N4O9
分子量：534.56
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CAS No: 87233-62-3
产品详情
生物活性：
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value 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.
体内研究：
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. Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B. Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs. Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM). Animal Model:Male ICR mice 5-6 weeks of age
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.
体外研究：
Emedastine difumarate inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM).High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts.Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration.
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value 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.
体内研究：
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. Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B. Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs. Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM). Animal Model:Male ICR mice 5-6 weeks of age
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.
体外研究：
Emedastine difumarate inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM).High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts.Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration.
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