| 溶解性 | 25°C: DMSO |
| 存贮条件 | 储存温度-20°C |
| 生化机理 | Description:IC50 Value: 127.5nM(Ki)[1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2]Ebrotidine is a competitive H2-receptor antagonist with a potent antisecretory activity and evidenced gastroprotection.in vitro: Ebrotidine displaced 3H-thiotidine specific binding to histamine H2-receptors (Ki: 127.5 nmol/l), showing a higher affinity (p < 0.05) than ranitidine (Ki: 190.0 nmol/l) and cimetidine (Ki: 246.1 nmol/l) [1].in vivo: Following intravenous administration to rats, ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner, ED50 being 0.21 and 0.44 mg/kg, respectively [2]. The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was significantly lower than that after placebo plus ASA (3.7 +/- 0.2). This reduction in lesion core by ebrotidine was accompanied by a significant increase in gastric blood flow (by 15% in corpus and 26% in antrum), by a rise in transmucosal potential difference (by 12%), and by a decrease of mucosal microbleeding [3]. Results of macroscopic assessment revealed that ebrotidine at doses of 50mg and higher/kg body weight effectively prevented mucosal injury, and that the maximal protective effect was achieved by 1h. Physicochemical analysis established that ebrotidine evoked 30% increase in mucus gel dimension, and showed 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%) [4].Clinical trial: N/A |
Ebrotidine,受体拮抗剂
Ebrotidine （订货以英文为准）
编号：E127604
CAS号：100981-43-9
分子式：C14H17BRN6O2S3
分子量：477.42
| 产品名称 | Ebrotidine |
| 中文名称 | Ebrotidine,受体拮抗剂 |
| CAS号 | 100981-43-9 |
| 分子式（M.F.） | C14H17BRN6O2S3 |
| 分子量（M.W.） | 477.42 |
| 储存条件 | -20°C储存 |
| RTECS | UT7937700 |
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