Kramer K, Bast A, Timmerman H
Agents Actions. 1987 Jun;21(1-2):41-8. doi: 10.1007/BF01974919.
The effects of the H2-receptor antagonists cimetidine, ranitidine, mifentidine and three analogues of mifentidine, were studied on the spontaneously beating right atrium (H2-antagonism) and membranes of the cerebral cortex (displacement of 3H-tiotidine), both obtained from the male guinea-pig. The choice of these compounds was based on preliminary experiments in which some mifentidine analogues were shown to displace tiotidine from the H2-receptor in a deviant manner. In the present study we investigated the relation between pharmacological response and receptor binding, also testing the degree of irreversible antagonism of these compounds in the atrium (functional) and cerebral cortex (binding) model. Our data indicate that a relation between the two different approaches for measuring the effect on the H2-receptor can be found, although some differences emerged as well.
研究了H2受体拮抗剂西咪替丁、雷尼替丁、米芬替丁以及米芬替丁的三种类似物对雄性豚鼠自发性搏动右心房（H2拮抗作用）和大脑皮质膜（3H-替奥替丁置换）的影响。选择这些化合物是基于初步实验，其中一些米芬替丁类似物显示出以异常方式从H2受体置换替奥替丁。在本研究中，我们研究了药理反应与受体结合之间的关系，还测试了这些化合物在心房（功能）和大脑皮质（结合）模型中的不可逆拮抗程度。我们的数据表明，尽管也出现了一些差异，但可以找到两种不同测量对H2受体影响方法之间的关系。
