Abstract
Analogs of the CCK-A receptor selective agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623) were prepared in which the lysine residue was replaced with L-4-aminophenylalanine and D-or L-3-aminophenylalanine. These new analogs were moderately potent antagonists of CCK-8 in the isolated guinea pig gallbladder with exceptional CCK-A receptor selectivity as evaluated in membrane preparations from CHO K1 cells stably transfected with human CCK-A and CCK-B receptors.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amino Acid Sequence
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Animals
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CHO Cells
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Cricetinae
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Gallbladder / drug effects
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Guinea Pigs
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Humans
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In Vitro Techniques
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Molecular Sequence Data
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Oligopeptides / chemical synthesis*
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Oligopeptides / pharmacology*
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Receptor, Cholecystokinin A
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Receptors, Cholecystokinin / antagonists & inhibitors*
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Receptors, Cholecystokinin / metabolism
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Tetragastrin / analogs & derivatives*
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Tetragastrin / chemical synthesis
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Tetragastrin / pharmacology
Substances
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Oligopeptides
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Receptor, Cholecystokinin A
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Receptors, Cholecystokinin
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Tetragastrin
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A 71623