Abstract
A series of 1,3,4-benzotriazepine-based CCK(2) antagonists have been devised by consideration of the structural features that govern CCK receptor affinity and the receptor subtype selectivity of 1,4-benzodiazepine-based CCK(2) antagonists. In contrast to the latter compounds, these novel 1,3,4-benzotriazepines are achiral, yet they display similar affinity for CCK(2) receptors to the earlier molecules and are highly selective over CCK(1) receptors.
MeSH terms
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Animals
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Benzazepines / chemical synthesis*
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Benzazepines / chemistry
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Benzazepines / pharmacology
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Benzodiazepines / chemistry
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Cell Line
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Cricetinae
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Cricetulus
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Crystallography, X-Ray
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Humans
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Mice
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Molecular Structure
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Radioligand Assay
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Rats
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Receptor, Cholecystokinin A / antagonists & inhibitors*
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Receptor, Cholecystokinin A / chemistry
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Receptor, Cholecystokinin B / antagonists & inhibitors*
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Receptor, Cholecystokinin B / chemistry
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Benzazepines
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Receptor, Cholecystokinin A
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Receptor, Cholecystokinin B
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Benzodiazepines
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Bz-423