Ebrotidine

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Background

Ebrotidine is a selective antagonist of histamine H2-receptor with Ki value of 127.5 nM [1]. Ebrotidine inhibited the secretion of gastric acid through competing with histamine for the combination with H2-receptor. It was found to have gastroprotective effect via abating the hyperplastic effects in gastric enteroendocrine cells and interfering the proteolytic and lipolytic activities and the urease of Helicobacter pylori. Besides that, ebrotidine promoted the proliferation of the epithelial cells and alleviated the effects brought by stress, ethanol and aspirin. Unlike other H2 inhibitors, ebrotidine showed no carcinogenic risk enterochromaffin-like cells of mice [1 and 2]. Ebrotidine showed about 10-fold higher anti-secretory effects than cimetidine. Its affinity for H2-receptor was 1.5- and 2-fold higher than that of ranitidine and cimetidine, respectively. In the in vitro assays, ebrotidine promoted the phospholipid secretion of gastric mucosa and maintained the calcium balance of mucosal cells through suppressing EGF-induced phosphorylation of calcium channel proteins. Ebrotidine exerted anti- Helicobacter pylori potency with MIC90 value of 256 mg/L. It inhibited 57% of the proteolytic activity and 93% of the lipolytic activity of the bacteria at concentrations of 35 and 60 mg/L, respectively. In addition, ebrotidine displayed inhibition effects on the urease at a low concentration of 2.1 μM by 77% [1]. The administration of 1 to 100 mg/kg ebrotidine dose-dependently inhibited gastric acid secretion in rats. The effects could last for about 8 hours when the dose was 100 mg/kg. Ebrotidine was also found to have the ability of helping healing ulcer [1].

[1]. Patel S S, Wilde M I. Ebrotidine. Drugs, 1996, 51(6): 974-80; discussion 981.
[2]. Romero A, Gómez F, Villamayor F, et al. Study of the population of enterochromaffin-like cells in mouse gastric mucosa after long-term treatment with ebrotidine. Toxicologic pathology, 1996, 24(2): 160-165.