Journal of Medicinal Chemistry · 1983 · 16 citations · 0 references
MedicineMedicinal ChemistryPharmacologyDrug DiscoveryGastrointestinal PharmacotherapyPharmacodynamicsCholinergic PharmacologyGastrointestinal PharmacologyAcid Secretion InhibitionGastric SecretionGastric Secretory PhysiologyGastrin SecretionHistamine H2 Receptor AntagonismHistamine Receptor AntagonismHistamine Receptor AntagonistsHistamine Receptor Pharmacology
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.