Impicciatore M, Chiavarini M, Razzetti R, Vitali T
Eur J Pharmacol. 1979 Jul 15;57(1):79-82. doi: 10.1016/0014-2999(79)90105-5.
Histamine and metiamide analogs with alkyl, methyl, ethyl or isopropyl groups on the imidazole ring in position 5, not previously tested on an in vivo preparation, were studied for their effects on gastric acid secretion in cats with gastric fistulas. Our findings confirmed that the methyl group appears to be optimal for an effect on gastric acid secretion as regards both agonism and antagonism. Ethyl substitution apparently did not change the pharmacological activity of histamine but modified the inhibitory effect of metiamide from competitive to non-competitive kinetics. Isopropyl analogs were inactive on gastric secretion under our experimental conditions.
研究了在5位咪唑环上带有烷基、甲基、乙基或异丙基的组胺和甲硫米特类似物，这些类似物此前未在体内制剂上进行过测试，研究它们对患有胃瘘的猫胃酸分泌的影响。我们的研究结果证实，就激动作用和拮抗作用而言，甲基似乎是对胃酸分泌产生影响的最佳基团。乙基取代显然没有改变组胺的药理活性，但将甲硫米特的抑制作用从竞争性动力学改变为非竞争性动力学。在我们的实验条件下，异丙基类似物对胃分泌无活性。
