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|Section2= }} Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine (Tagamet). ==Development of metiamide from burimamide== After discovering that burimamide is largely inactive at physiological pH, due to the presence of its electron donating side chain, the following steps were undertaken to stabilize burimamide: *addition of a sulfide group close to the imidazole ring, giving thiaburimamide *addition of methyl group to the 4- position on the imidazole ring to favour the tautomer of thiaburimamide which binds better to the H2-receptor These changes increased the bioavailability metiamide so that it is 10 times more potent than burimamide in inhibiting histamine-stimulated release of gastric acid.〔 The clinical trials that began in 1973 demonstrated the ability of metiamide to provide symptomatic relief for ulcerous patients by increasing healing rate of peptic ulcers. However, during these trials, an unacceptable number of patients dosed with metiamide developed agranulocytosis (decreased white blood cell count).〔 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「metiamide」の詳細全文を読む スポンサード リンク
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