The substituted benzamide derivative zacopride was found to antagonize competitively the effects of 5-hydroxytryptamine (5-HT) on the guinea-pig ileum, the rabbit vagus nerve and the von Bezold Jarisch reflex in the rat. The potency of zacopride was comparable with that of ICS 205-930 and it is concluded that zacopride possesses 5-HT3 receptor antagonizing properties.
The H2-receptor antagonists have undoubtably been successful in healing primary gastric and duodenal ulcers so there is a tendency to assume that they will be equally successful when used as prophylactic agents. When used to prevent gastroduodenal ulceration induced by nonsteroidal anti-inflammatory agents, they are unsuccessful in protecting against gastric damage, but reduce the incidence of duodenal ulceration. However, their effect on the incidence of serious complications remains unknown. In the prevention of stress ulceration and bleeding in intensive care units there is evidence of a beneficial effect of H2-receptor antagonists, but other agents are also equally effective. In patients who present with haematemesis and melaena, there is little evidence to show that H2-receptor antagonists reduce rates of transfusion or surgical intervention, or decrease mortality.
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