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New glutaramic acid derivatives with potent competitive and specific cholecystokinin-antagonistic activity.
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1985
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Gastrointestinal PharmacologyGastroenterologyPharmacotherapyExperimental PharmacologyGastrointestinal Peptide HormoneMolecular PharmacologyMedicinal ChemistryBinding SiteDerivativesBiochemistryMedicinePharmacological AgentPharmacologyGuinea Pig GallbladderBiliary TractNatural SciencesCumulative Dose-response CurveSpecific Cholecystokinin-antagonistic ActivityDrug Discovery
New glutaramic acid derivatives were evaluated for anti-cholecystokinin (CCK) activity in vitro on guinea pig gallbladder. The compounds are competitive and specific CCK-antagonists, causing a parallel right shift of the cumulative dose-response curve of the agonist. The affinity for the binding site of the CCK-receptor for some of these compounds was hundreds of times higher than that of pro-glumide, the model compound.