依美司丁
| 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;杂质对照品;原料药;impurity |
| Mol文件 | 87233-61-2.mol |
| 结构式 |  |
依美司丁 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（413.35mM）；乙醇：100 mg/ml（330.68 mM） |
| 酸度系数(pKa) | 8.86±0.10(Predicted) |
| CAS 数据库 | 87233-61-2(CAS DataBase Reference) |
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。
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。| Target | Value |
|
H1 receptor
(Cell-free assay) | 1.3 nM(Ki) |
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.
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-108411 | Emedastine | 1 mg | 288元 | |
| 2024/01/25 | HY-108411 | 依美司丁 Emedastine | 87233-61-2 | 5mg | 720元 |