富马酸依美斯汀

生物活性靶点体外研究体内研究富马酸依美斯汀试剂级价格

富马酸依美斯汀

CAS号:87233-62-3
英文名:EMEDASTINE FUMARATE
中文名:富马酸依美斯汀
CBNumber:CB6714475
分子式:C25H34N4O9
分子量:534.56
MOL File:87233-62-3.mol

富马酸依美斯汀化学性质

熔点 :148-151°
储存条件 :2-8°C
溶解度 :Soluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in acetone.
Merck :14,3557

安全信息

RTECS号 :DD8870000
海关编码 :2933992600
毒性 :LD50 orally in guinea pigs: 744 mg/kg (Fukuda)

富马酸依美斯汀性质、用途与生产工艺

生物活性 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。
靶点
Target Value
Histamine H1 receptor
()
体外研究

Emedastine difumarate inhibits histamine H ₂ receptor (K _i =49067 nM) and histamine H ₃ receptor (K _i =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.

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 (IC ₅₀ =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.