Abstract
A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTH1R) antagonist. A process of optimization afforded derivatives displaying nanomolar PTH1R affinity, a representative example of which behaved as a PTH1R antagonist in cell-based cyclic adenosine monophosphate (cAMP) assays, with selectivity over PTH2 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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Binding, Competitive
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Cell Line
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Cell Line, Tumor
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Cricetinae
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Cricetulus
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Cyclic AMP / biosynthesis
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Humans
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Mice
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Radioligand Assay
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Receptor, Parathyroid Hormone, Type 1 / antagonists & inhibitors*
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Recombinant Proteins / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Benzazepines
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Receptor, Parathyroid Hormone, Type 1
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Recombinant Proteins
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Cyclic AMP