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Samuel Vaisrub, MD

JAMA. 1976;235(18):2006-2007.

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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 ( 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 . . . [Full Text PDF of this Article]

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