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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
18
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pubmed:dateCreated |
1986-12-3
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pubmed:abstractText |
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 of peripheral CCK antagonists.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepinones,
http://linkedlifedata.com/resource/pubmed/chemical/Cholecystokinin,
http://linkedlifedata.com/resource/pubmed/chemical/Devazepide,
http://linkedlifedata.com/resource/pubmed/chemical/Proglumide,
http://linkedlifedata.com/resource/pubmed/chemical/Sincalide,
http://linkedlifedata.com/resource/pubmed/chemical/asperlicin,
http://linkedlifedata.com/resource/pubmed/chemical/lorglumide
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0024-3205
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
3
|
pubmed:volume |
39
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1631-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3773639-Administration, Oral,
pubmed-meshheading:3773639-Animals,
pubmed-meshheading:3773639-Benzodiazepinones,
pubmed-meshheading:3773639-Binding, Competitive,
pubmed-meshheading:3773639-Cholecystokinin,
pubmed-meshheading:3773639-Devazepide,
pubmed-meshheading:3773639-Dose-Response Relationship, Drug,
pubmed-meshheading:3773639-Female,
pubmed-meshheading:3773639-Gastric Emptying,
pubmed-meshheading:3773639-Mice,
pubmed-meshheading:3773639-Proglumide,
pubmed-meshheading:3773639-Sincalide,
pubmed-meshheading:3773639-Time Factors
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pubmed:year |
1986
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pubmed:articleTitle |
A new simple mouse model for the in vivo evaluation of cholecystokinin (CCK) antagonists: comparative potencies and durations of action of nonpeptide antagonists.
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pubmed:publicationType |
Journal Article,
Comparative Study
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