Abstract
A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the series, and further fine tuning of the affinity results in CCK1R selectivity of greater than 100-fold.
MeSH terms
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Animals
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Benzamides / pharmacology
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Cloning, Molecular
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Drug Evaluation, Preclinical
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Genotype
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Isoxazoles / chemistry*
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Maze Learning
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Models, Molecular
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Rats
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Rats, Sprague-Dawley
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Receptor, Cholecystokinin A / antagonists & inhibitors*
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Receptor, Cholecystokinin A / genetics
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Receptor, Cholecystokinin A / metabolism
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Receptor, Cholecystokinin B / antagonists & inhibitors*
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Receptor, Cholecystokinin B / genetics
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Receptor, Cholecystokinin B / metabolism
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Structure-Activity Relationship
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Sulfonamides / pharmacology*
Substances
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Benzamides
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Isoxazoles
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Receptor, Cholecystokinin A
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Receptor, Cholecystokinin B
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Sulfonamides
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anthranil
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benzamide