中文名 | 依美司丁 |
英文名 | Emedastine |
别名 | 依美司丁 依美斯汀 依美斯汀杂质D 依美斯汀杂质E 依美斯汀杂质F 依美斯汀杂质B 依美斯汀杂质C 1-(2-乙氧基乙基)-2-(4-甲基-1,4-二氮杂庚烷-1-基)苯并咪唑 |
英文别名 | Rapimine Emedastine EMEDASTINE 87233-61-2 Emedastine impurity F 1-(2-Ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)benzimidazole 1-[2-(Ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole 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-1,3-benzodiazole 1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole 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 1H-benzimidazole, 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)- 1-(2-Ethoxyethyl)-2-[(hexahydro-4-methyl-1H-1,4-diazepin)-1-yl]-1H-benzimidazole |
CAS | 87233-61-2 |
EINECS | 200-258-5 |
化学式 | C17H26N4O |
分子量 | 302.41 |
InChI | InChI=1/C17H26N4O/c1-3-22-14-13-21-16-8-5-4-7-15(16)18-17(21)20-10-6-9-19(2)11-12-20/h4-5,7-8H,3,6,9-14H2,1-2H3 |
密度 | 1.15±0.1 g/cm3(Predicted) |
沸点 | 446.6±55.0 °C(Predicted) |
闪点 | 223.9°C |
蒸汽压 | 3.59E-08mmHg at 25°C |
折射率 | 1.594 |
酸度系数 | 8.86±0.10(Predicted) |
存储条件 | 2-8°C |
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. |
上游原料 | N1-(2-乙氧基乙基)苯-1,2-二胺 依美司汀 EP 杂质 E 1,4-二氮杂环庚烷-1-甲酸叔丁酯 N-甲基高哌嗪 2-氯苯并咪唑 苯胺 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.307 ml | 16.534 ml | 33.068 ml |
5 mM | 0.661 ml | 3.307 ml | 6.614 ml |
10 mM | 0.331 ml | 1.653 ml | 3.307 ml |
5 mM | 0.066 ml | 0.331 ml | 0.661 ml |
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