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• 产品描述： Ebrotidine is a competitive H2-receptor antagonist with Ki of 127.5 nM. Ebrotidine has a potent antisecretory activity and evidenced gastroprotection.

• 靶点： Histamine Receptor;HistamineReceptor

• 体内研究：
  Ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner (ED50: 0.21 and 0.44 mg/kg, respectively), following intravenous administration to rats. Results of the 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 a 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%). The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was obviously 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 micro bleeding

• 参考文献：
  1. Agut J, Sánchez JC, Sacristán A, Action of ebrotidine, ranitidine and cimetidine on the specific binding to histamine H1- and H2-receptors. Arzneimittelforschung. 1997 Apr;47(4A):447-9. 2. Piotrowski J, Yamaki K, Morita M, Ebrotidine--a new H2-receptor antagonist with mucosal strengthening activity. Biochem Int. 1992 Mar;26(4):659-67. 3. Konturek SJ, Kwiecien N, Sito E, Effects of ebrotidine on aspirin-induced gastric mucosal damage and blood flow in humans. Scand J Gastroenterol. 1993 Dec;28(12):1047-50. 4. Palop D, Agut J, Márquez M, Histamine H2-receptor antagonist action of ebrotidine. Effects on gastric acid secretion, gastrin levels and NSAID-induced gastrotoxicity in the rat. Arzneimittelforschung. 1997 Apr;47(4A):439-46.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.095 ml	10.473 ml	20.946 ml
  5 mM	0.419 ml	2.095 ml	4.189 ml
  10 mM	0.209 ml	1.047 ml	2.095 ml
  50 mM	0.042 ml	0.209 ml	0.419 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *