Key result
Zafirlukast significantly reduced DDAVP-dependent cAMP production and water reabsorption in vitro, demonstrating potential as a repurposed V2R antagonist with effects comparable to tolvaptan.
Why the study?
The study aimed to identify existing drugs that could be repurposed as antagonists of the vasopressin V2 receptor, a GPCR controlling renal water balance and involved in abnormal cell proliferation, cancer, and renal cyst enlargement.
Population
1882 existing drugs screened and renal collecting duct MCD4 cells stably expressing human V2R and AQP2
Comparison
Prioritized candidate drugs vs tolvaptan
Design
AI-based reverse screening and in vitro experimental validation study
Authors
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Requires experimental validation before any clinical use; leaves open V2R antagonist repurposing pending prospective studies.
AI-driven screening and in vitro testing identified zafirlukast as a novel and potent vasopressin V2 receptor antagonist.
Trisciuzzi et al. (2025) studied V2R antagonism. Zafirlukast vs. Tolvaptan was evaluated on DDAVP-dependent cAMP production and water reabsorption. Zafirlukast significantly reduced DDAVP-dependent cAMP production and water reabsorption in vitro, demonstrating potential as a repurposed V2R antagonist with effects comparable to tolvaptan.
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