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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：C14H17N6O2S3BR
分子量：477.42
货号 品牌 包装 目录价 您的价格 库存 数量 购买
E127604-50mg 阿拉丁 50mg ¥2682.90
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E127604-10mg 阿拉丁 10mg ¥804.90
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E127604-5mg 阿拉丁 5mg ¥511.90
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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.） C14H17N6O2S3BR
分子量（M.W.） 477.42
储存条件 -20°C储存
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
RTECSUT7937700
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