Bertaccini G, Coruzzi G
Naunyn Schmiedebergs Arch Pharmacol. 1981 Nov;317(3):225-7. doi: 10.1007/BF00503821.
Several histamine H2-receptor antagonists (cimetidine, ranitidine, oxmetadine and tiotidine) were tested for their activity on the papillary muscle of the guinea pig stimulated by histamine. All of the compounds exerted a competitive antagonism against histamine the order of potency being tiotidine greater than oxmetidine greater than ranitidine greater than cimetidine. Oxmetidine was the only drug which at high concentrations (10-6 M) decreased in maximum response of histamine probably because of non specific effects of the molecule already described in the literature. As it was expected, the H1-receptor antagonist, mepyramine, exerted a non-competitive antagonism.
测试了几种组胺H2受体拮抗剂（西咪替丁、雷尼替丁、奥美替丁和替奥替丁）对组胺刺激的豚鼠乳头肌的活性。所有化合物均对组胺产生竞争性拮抗作用，效力顺序为替奥替丁＞奥美替丁＞雷尼替丁＞西咪替丁。奥美替丁是唯一一种在高浓度（10-6 M）时降低组胺最大反应的药物，这可能是由于文献中已描述的该分子的非特异性作用。正如预期的那样，H1受体拮抗剂美吡拉敏产生非竞争性拮抗作用。
