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May 3, 1976

Histamine H2 Receptor-Antagonists

JAMA. 1976;235(18):2006-2007. doi:10.1001/jama.1976.03260440058030

Histamine H2 receptor-antagonists—burimamide, metiamide, cimetidine—are currently arousing much anticipatory excitement. The relatively recent concept that there is more than one receptor for histamine is based on the observation that pyrilamine (mepyramine) and other, older antihistamines have no effect on histamine-mediated secretion of gastric acid or on the heart rate. Intrigued by this observation and mindful of the analogous situation that existed in the field of catecholamines before adrenergic receptors were shown to be of two kinds (α and β), Black and his colleagues1 in 1964 began to synthesize and test potential inhibitors of another histamine receptor that may be involved in pyrilamine-insensitive responses. Their work culminated in precise definition of the pyrilamine-sensitive H1 and pyrilamine-insensitive H2 receptors and in the synthesis of burimamide,1 the first of the synthetic H2 receptor-antagonists.

Burimamide, which is more effective intravenously than orally, and the subsequently synthesized metiamide and