依美司丁

简介生物活性靶点体外研究体内研究依美司丁试剂级价格

依美司丁

CAS号:87233-61-2
英文名:Emedastine
中文名:依美司丁
CBNumber:CB8728076
分子式:C17H26N4O
分子量:302.41
MOL File:87233-61-2.mol

依美司丁化学性质

沸点 :446.6±55.0 °C(Predicted)
密度 :1.15±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO: 125 mg/mL (413.35 mM); Ethanol: 100 mg/mL (330.68 mM)
酸度系数(pKa) :8.86±0.10(Predicted)
形态 :Viscous Liquid
颜色 :Yellow to brown
CAS 数据库 :87233-61-2(CAS DataBase Reference)

依美司丁性质、用途与生产工艺

简介
依美斯汀（Emedastine，商品名称： Emadine）是第二代抗组织胺，可用作眼药水以减缓过敏性结膜炎的症状。依美斯汀属于H1 接收器抑制剂。借由抑制组织胺的作用来减缓过敏性结膜炎的症状。当依美斯汀用作眼药水时，会以双延胡索酸盐（difumarate）的形式存在。
生物活性 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，Ki 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。
靶点
Target Value
H1 receptor
(Cell-free assay) 1.3 nM(Ki)
体外研究

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

体内研究

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 (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.