Norris D B, Gajtkowski G A, Wood T P, Rising T J
Agents Actions. 1985 Apr;16(3-4):170-2. doi: 10.1007/BF01983130.
Thirty-seven compounds were evaluated for their ability to inhibit histamine stimulated adenylate cyclase and to inhibit 3H-tiotidine binding. The compounds examined included a number of known H2-antagonists and a number of potential H2-antagonists of diverse chemical structure. The correlation between the Ki values from the binding assay and from the inhibition of adenylate cyclase was calculated to be r = 0.99, p less than 0.001. Thus 3H-tiotidine binding in guinea-pig cerebral cortex can be used to give a valid assessment of histamine H2-receptor activity.
对37种化合物抑制组胺刺激的腺苷酸环化酶的能力以及抑制3H-替丁结合的能力进行了评估。所检测的化合物包括一些已知的H2拮抗剂和一些具有不同化学结构的潜在H2拮抗剂。结合试验和腺苷酸环化酶抑制试验所得Ki值之间的相关性经计算为r = 0.99，p小于0.001。因此，豚鼠大脑皮层中的3H-替丁结合可用于对组胺H2受体活性进行有效评估。
