PMID: 3773639Nov 3, 1986Paper

A new simple mouse model for the in vivo evaluation of cholecystokinin (CCK) antagonists: comparative potencies and durations of action of nonpeptide antagonists

Life Sciences
V J LottiR S Change

Abstract

A new simple mouse assay for the in vivo evaluation of CCK antagonists which is based upon visual determination of the gastric emptying of a charcoal meal is described. CCK-8 (24 micrograms/kg s.c.) but not various other peptide and nonpeptide agents effectively inhibited gastric emptying in this test system. The effect of CCK-8 was antagonized by established peripheral CCK antagonists but not representative agents of various other pharmacological classes. The rank order of potency of the CCK antagonists were: L-364,718 (ED50 = 0.01 mg/kg, i.v.; 0.04 mg/kg, p.o.) greater than Compound 16 (ED50 = 1.5 mg/kg, i.v.; 2.0 mg/kg p.o.) greater than asperlicin (ED50 = 14.8 mg/kg i.v.) greater than proglumide (ED50 = 184 mg/kg i.v.; 890 mg/kg, p.o.). Duration of action studies based upon ED50 values determined at various time intervals after oral administration showed that L-364,718 and proglumide are considerably longer acting than Compound 16. Asperlicin (ED50 greater than 300 mg/kg, p.o.) was ineffective as a CCK antagonist when administered orally. These data provide the first direct comparisons of the in vivo potencies of current CCK antagonists and demonstrate the utility of a new simple mouse assay for the in vivo characterization...Continue Reading

References

Jan 1, 1982·Pharmacology·H Kilbinger, T R Weihrauch

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Citations

Jun 3, 1999·European Journal of Clinical Investigation·A C García-MonteroI De Dios
Sep 18, 1997·Proceedings of the National Academy of Sciences of the United States of America·M D BarrachinaY Taché
Jun 1, 1995·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·M Karaus, C Niederau
Dec 1, 1993·The Journal of Pharmacy and Pharmacology·N J BrownN W Read
Jun 5, 2004·Regulatory Peptides·Charlotta Dornonville de la CourRolf Håkanson
Oct 27, 2004·Advances in Protein Chemistry·Elaine K LauTracy M Handel
Sep 1, 1991·International Journal of Pancreatology : Official Journal of the International Association of Pancreatology·T Takács, A Pap

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