Abstract
The synthesis of lipophylic derivatives of the amino acid residues of the CCK-8 fragment is described. According to "in vitro" binding studies and functional test, nearly all the compounds behaves as CCK-antagonists; moreover some compounds are able to interact differentially with CCK-A and CCK-B receptor subtype. In particular, compounds 2c, 2g, and 2h possess a high affinity for the CCK-A receptor subtype coupled with a low affinity for the CCK-B subtype. This results in an interesting selectivity profile. However, the same compounds are not able to antagonize the effects exerted by CCK-itself, when tested in "in vivo" assays.
MeSH terms
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Amino Acid Sequence
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Animals
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Brain Chemistry / drug effects
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Cholecystokinin / antagonists & inhibitors*
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Female
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Gallbladder / drug effects
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Guinea Pigs
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In Vitro Techniques
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Male
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Mice
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Molecular Sequence Data
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Pancreas / drug effects
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Pancreas / metabolism
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Pyrazines / chemical synthesis*
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Pyrazines / pharmacology
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Pyrazines / therapeutic use
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Receptors, Cholecystokinin / antagonists & inhibitors*
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Sincalide / analogs & derivatives*
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Sincalide / pharmacology
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Thiones / chemical synthesis
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Thiones / pharmacology
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Thiones / therapeutic use
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Thiophenes
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Vinyl Compounds / chemical synthesis*
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Vinyl Compounds / pharmacology
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Vinyl Compounds / therapeutic use
Substances
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Pyrazines
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Receptors, Cholecystokinin
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Thiones
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Thiophenes
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Vinyl Compounds
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oltipraz
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Cholecystokinin
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Sincalide