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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1990-3-9
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pubmed:abstractText |
Novel aryl amide analogues of glutamic acid dialkylamide have been synthesized to test for a possible structural analogy between glutamic acid and benzodiazepine CCK antagonists such as compounds 2 and 24 (lorglumide and MK-329, respectively). In support of the structural model, certain of these hybrid compounds are more potent in pancreas CCK radioligand binding assays than corresponding lorglumide-type reference compounds. Modifications previously found in the benzodiazepine antagonists to result in brain CCK/gastrin receptor selectivity were also incorporated to produce an aryl urea series of glutamic acid analogues. None of these compounds were brain CCK/gastrin selective; however, one was potent and selective in the pancreas binding assay. The model appears to be most useful in the design of selective ligands for the pancreas type CCK receptor.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
33
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
591-5
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:2299627-Animals,
pubmed-meshheading:2299627-Brain,
pubmed-meshheading:2299627-Chemical Phenomena,
pubmed-meshheading:2299627-Chemistry,
pubmed-meshheading:2299627-Chemistry, Physical,
pubmed-meshheading:2299627-Cholecystokinin,
pubmed-meshheading:2299627-Computer Graphics,
pubmed-meshheading:2299627-Glutamates,
pubmed-meshheading:2299627-Guinea Pigs,
pubmed-meshheading:2299627-Ligands,
pubmed-meshheading:2299627-Models, Molecular,
pubmed-meshheading:2299627-Molecular Conformation,
pubmed-meshheading:2299627-Pancreas,
pubmed-meshheading:2299627-Physicochemical Phenomena,
pubmed-meshheading:2299627-Rats,
pubmed-meshheading:2299627-Receptors, Cholecystokinin,
pubmed-meshheading:2299627-Structure-Activity Relationship
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pubmed:year |
1990
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pubmed:articleTitle |
Novel glutamic acid derived cholecystokinin receptor ligands.
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pubmed:affiliation |
Merck Sharp & Dohme Research Laboratories, West Point, Pennsylvania 19486.
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pubmed:publicationType |
Journal Article
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