87233-61-2
87233-61-2 结构式
基本信息
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
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
物理化学性质
常见问题列表
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。
| 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. |