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Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives
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1983
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Gastrointestinal PharmacologyGastric Acid SecretionGastroenterologyPharmacotherapyExperimental PharmacologyPharmaceutical ChemistryGastrointestinal Peptide HormoneMedicinal ChemistryAllergyBiochemistryAminoalkyl-substituted PyridylureasPharmacologyHistamine H2 ReceptorNatural SciencesPhysiologyAnesthesiaMedicineDrug DiscoveryH2 Receptor
A series of aminoalkyl-substituted pyridylureas has been prepared and evaluated as inhibitors of gastric acid secretion. N,N-Dimethyl-N'-[2-(diisopropylamino)ethyl]-N'-(4,6-dimethyl-2-pyridyl)urea (8g) was the most potent example of the class. Comparison of this compound with cimetidine showed it to be equipotent in dogs stimulated with gastrin tetrapeptide but approximately half as potent in dogs stimulated with histamine. Inhibition of secretion does not appear to result from antagonism of the histamine H2 receptor, since the compounds show only weak inhibition of the H2 receptor in vitro.