Morini G, Plazzi P V, Bordi F, Impicciatore M
Boll Soc Ital Biol Sper. 1980 Jan 15;56(1):88-94.
In the present paper the authors describe the effects of Dimaprit analogs on guinea pig gastric mucosa "in vitro". This preparation, widely described by Holton and Spencer, is useful for studying the actions of stimulants and inhibitors which act directly on the oxyntic cells. Such compounds are weakly active as stimulants of H2-receptors and studied as antagonists fail in inhibiting acid secretion evoked by Dimaprit, the most specific H2-receptors agonist. In particular, the compound marked Ros 5 clarifies that the isothiourea group of Dimaprit simulates the amidine system only chemically but not pharmacologically. The different mechanism of Dimaprit and Histamine on H2-receptors has been discussed.
在本论文中,作者描述了二甲双胍类似物对豚鼠胃黏膜的“体外”作用。这种制剂被霍尔顿和斯宾塞广泛描述,可用于研究直接作用于壁细胞的兴奋剂和抑制剂的作用。这类化合物作为H2受体兴奋剂活性较弱,作为拮抗剂研究时,无法抑制由最特异的H2受体激动剂二甲双胍诱发的胃酸分泌。特别是标记为Ros 5的化合物表明,二甲双胍的异硫脲基团仅在化学上模拟脒系统,而非药理学上。文中还讨论了二甲双胍和组胺在H2受体上的不同作用机制。