| Hazard Information | Back Directory | [Description]
DA 4626 is H2-receptor antagonism. The compounds which were investigated in a wider concentration range, i.e. DA 4360, DA 4577, and DA 4626, behaved as simple competitive antagonists, yielding apparent KB values comparable with those estimated in conventional H2-receptor assays. These results provide further evidence for the highly selective H2-receptor antagonism of these new molecules, and confirm the suitability of the histamine-stimulated adenylate cyclase assay in guinea-pig gastric cells as a functionally reduced system for the study of H2 antagonists. | [Uses]
DA 4626 is a competitive H2-histamine receptor antagonist. DA 4626 inhibits adenylate cyclase activity with a KB value of 40 nM[1]. | [IC 50]
H2 Receptor; adenylate cyclase: 40 nM (Kb) | [References]
[1] Micheletti R, et al. Evaluation of novel compounds interacting with H2-histamine receptors: effect on histamine-sensitive adenylate cyclase activity in guinea-pig gastric mucosa. Agents Actions. 1985 Jul;16(5):291-4. DOI:10.1007/BF01982860 |
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