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
- 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
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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。
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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.
- 更新日期：2024/11/08
- 产品编号：HY-108411
- 产品名称：Emedastine
- CAS编号：
- 包装：1 mg
- 价格：288元
- 更新日期：2024/11/08
- 产品编号：HY-108411
- 产品名称：依美司丁 Emedastine
- CAS编号：87233-61-2
- 包装：5mg
- 价格：720元
- 公司名称：Alsachim SAS
- 联系电话：--
- 电子邮件：sales@alsachim.com
- 国家：法国
- 产品数：424
- 优势度：0
