New Histamine Antagonists

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Abstract
The 1st H2-receptor antagonist, burimamide, has been superseded in pharmacological and clinical evaluation by metiamide which is more potent and less toxic. Metiamide produces a marked inhibition of both the volume and the concentration of gastric acid secretion induced by food, histamine, pentagastrin, vagal stimulation and all the methyl derivatives of histamine. Metiamide thus appears to be a universal gastric secretory inhibitor and at present 2, as yet unresolved, theories predominate as to how this is achieved: the drug may block the action of histamine acting as the final common local chemostimulator of the parietal cells; or the 3 major agonists histamine, gastrin and acetylcholine, may each bind to a specific receptor site on the parietal cell and blockade of 1 receptor may modify the response of 1 or both the other receptors to their respective agonists.