Perrier C V, Griessen M
Eur J Clin Invest. 1976 Jan 30;6(1):113-20. doi: 10.1111/j.1365-2362.1976.tb00500.x.
In the guinea-pig, it has been shown that homogenates of mucosa from the fundus contain an adenylyl cyclase system that is activated by histamine as well as by prostaglandins PGE1 and PGA1. The effects of burimamide, an H2-inhibitor, and mepyramine and chlorpheniramide, both H1-inhibitors, were tested. Both H1 and H2 inhibitors behaved kinetically as competitive inhibitors of histamine, but the Km derived for burimamide (2.5 - 4.1 . 10(-5)) was significantly lower than that for either chlorpheniramine (0.9 - 1.9 . 10(-4)) or mepyramine (1.3 - 1.4 . 10(-4)). On the other hand none of the three inhibitors influenced the cyclase activation by PGE1 and PGA1. These results suggest that there are at least two types of receptors in the preparation studied, one responsive to histamine and the other to the prostaglandins, and that the specificity of H1- and H2-receptors is not absolute in the broken cell preparation.
在豚鼠中，已表明胃底部黏膜匀浆含有一种腺苷酸环化酶系统，该系统可被组胺以及前列腺素PGE1和PGA1激活。测试了H2抑制剂布立马胺以及H1抑制剂美吡拉敏和氯苯那敏的作用。H1和H2抑制剂在动力学上均表现为组胺的竞争性抑制剂，但布立马胺的Km值（2.5 - 4.1×10⁻⁵）显著低于氯苯那敏（0.9 - 1.9×10⁻⁴）或美吡拉敏（1.3 - 1.4×10⁻⁴）。另一方面，这三种抑制剂均不影响PGE1和PGA1对环化酶的激活。这些结果表明，在所研究的制剂中至少存在两种类型的受体，一种对组胺有反应，另一种对前列腺素有反应，并且在破碎细胞制剂中H1和H2受体的特异性并非绝对。
