EBROTIDINE, A NOVEL H-2-RECEPTOR ANTAGONIST WITH LOCAL GASTROPROTECTIVE ACTIVITY

Ebrotidine is a new H-2-receptor antagonist with gastric inhibitory and protective activities. This study was designed to compare the gastric inhibitory and gastroprotective effects of ebrotidine with those of ranitidine against mucosal damage induced by ethanol, aspirin (ASA), taurocholate and stress and to elucidate the mechanism of action, especially the role of mucosal blood flow and mucosal formation of prostaglandins. It was found that intragastric ebrotidine has gastric inhibitory action similar to ranitidine on acid and pepsin secretion in chronic gastric fistula rats. Ebrotidine, like ranitidine, probably prevented gastric lesions induced by ASA, taurocholate or stress by inhibiting gastric secretion. Unlike ranitidine, intragastric ebrotidine protected gastric mucosa against acute damage by absolute ethanol and this effect was accompanied by an increase in mucosal blood flow and prostaglandin biosynthesis. This suggests that ebrotidine possesses unique local gastroprotective activity mediated, at least in part, by increased gastric mucosal microcirculation and prostaglandin formation.