Benzodiazepine Derivatives as Potent Vasopressin V2 Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease

Abstract excerpt

Cyst formation and enlargement in autosomal dominant kidney disease (ADPKD) is mainly driven by aberrantly increased cytosolic cAMP in renal tubule epithelial cells. Because the vasopressin V 2 receptor (V 2 R) regulates intracellular cAMP levels in kidneys, a series of benzodiazepine derivatives were developed targeting the V 2 R. Among these derivatives, compound 25 exhibited potent binding affinity to the V 2...

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