中文名称:

依美司丁

中文同义词:

依美司丁;依美斯汀;1-(2-乙氧基乙基)-2-(4-甲基-1,4-二氮杂庚烷-1-基)苯并咪唑;依美斯汀杂质B;依美斯汀杂质C;依美斯汀杂质D;依美斯汀杂质E;依美斯汀杂质F

英文名称:

Emedastine

英文同义词:

EMEDASTINE;1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole;1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepine-1-yl)-1H-benzimidazole;1-(2-Ethoxyethyl)-2-[(hexahydro-4-methyl-1H-1,4-diazepin)-1-yl]-1H-benzimidazole;1-(2-ethoxyethyl)-2-(4-Methyl-1,4-diazepan-1-yl)-1H-1,3-benzodiazole;1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzimidazole;1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole;Emedastine impurity F

CAS号:

87233-61-2

分子式:

C17H26N4O

分子量:

302.41

EINECS号:

200-258-5

相关类别:

杂质世界-依美斯汀;impurity

Mol文件:

87233-61-2.mol

沸点 

446.6±55.0 °C(Predicted)

密度 

1.15±0.1 g/cm3(Predicted)

储存条件 

Sealed in dry,2-8°C

酸度系数(pKa)

8.86±0.10(Predicted)

CAS 数据库

87233-61-2(CAS DataBase Reference)

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)

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.

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.