The use of an in vitro binding assay to predict histamine H2-antagonist activity
- PMID: 2861729
- DOI: 10.1007/BF01983130
The use of an in vitro binding assay to predict histamine H2-antagonist activity
Abstract
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.
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