Brimblecombe R W, Duncan W A, Owen D A, Parsons M E
Fed Proc. 1976 Jun;35(8):1931-4.
Burimamide and metiamide are two histamine H2-receptor antagonists. Evidence is presented that indicates the competitive nature and the specificity of the antagonism. Metiamide is about ten times more potent than burimamide and is also more effective than burimamide when given orally. Both compounds inhibit gastric secretion and the evidence is consistent with this inhibition being due to competitive antagonism of H2 receptors in the gastric mucosa. Burimamide, unlike metiamide, causes release of catecholamines even at dose levels that are just sufficient to produce H2-receptor antagonism. Burimamide, but not metiamide, has alpha-adrenoceptor blocking activity. In certain models for inflammation, particularly rat paw edema induced by compound 48/80, burimamide in combination with the H1-receptor antagonist mepyramine shows anti-inflammatory activity. This may, in part, be associated with the catecholamine-releasing properties of the compound. Metiamide is less active in this respect.
布立马胺和甲硫米特是两种组胺H2受体拮抗剂。现有证据表明了这种拮抗作用的竞争性本质和特异性。甲硫米特的效力约为布立马胺的十倍，口服时也比布立马胺更有效。两种化合物均抑制胃酸分泌，且证据表明这种抑制作用是由于对胃黏膜中H2受体的竞争性拮抗所致。与甲硫米特不同，布立马胺即使在仅足以产生H2受体拮抗作用的剂量水平下也会引起儿茶酚胺释放。布立马胺具有α-肾上腺素能受体阻断活性，而甲硫米特没有。在某些炎症模型中，特别是由化合物48/80诱导的大鼠足爪水肿模型中，布立马胺与H1受体拮抗剂美吡拉敏联合使用时显示出抗炎活性。这可能部分与该化合物的儿茶酚胺释放特性有关。甲硫米特在这方面活性较低。
