Nielsen S T
Pharmacology. 1987;34(1):25-9. doi: 10.1159/000138244.
Histamine, acting through H2 receptors, increases cAMP formation in homogenates of guinea pig hippocampus. The activities of two H2 antagonists, tiotidine and ICIA 5165, as inhibitors of the histamine-induced increase were investigated. ICIA 5165 and tiotidine were potent antagonists of histamine with a pKi of 8.0 and 7.6, respectively. Similarly, the positive chronotropic response of isolated guinea pig atria to histamine was antagonized by tiotidine and ICIA 5165 with a pKB of 7.8 and 7.9, respectively. These studies suggest that histamine H2 receptors in the CNS and atria are similar.
组胺通过H2受体发挥作用，可增加豚鼠海马匀浆中cAMP的生成。研究了两种H2拮抗剂噻替丁和ICIA 5165作为组胺诱导增加的抑制剂的活性。ICIA 5165和噻替丁是组胺的强效拮抗剂，其pKi分别为8.0和7.6。同样，噻替丁和ICIA 5165分别以pKB 7.8和7.9拮抗离体豚鼠心房对组胺的正性变时反应。这些研究表明，中枢神经系统和心房中的组胺H2受体相似。
