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• W2145910029 abstract "Urea transport (UT) proteins facilitate the concentration of urine by the kidney, suggesting that inhibition of these proteins could have therapeutic use as a diuretic strategy. We screened 100,000 compounds for UT-B inhibition using an optical assay based on the hypotonic lysis of acetamide-loaded mouse erythrocytes. We identified a class of triazolothienopyrimidine UT-B inhibitors; the most potent compound, UTBinh-14, fully and reversibly inhibited urea transport with IC50 values of 10 nM and 25 nM for human and mouse UT-B, respectively. UTBinh-14 competed with urea binding at an intracellular site on the UT-B protein. UTBinh-14 exhibited low toxicity and high selectivity for UT-B over UT-A isoforms. After intraperitoneal administration of UTBinh-14 in mice to achieve predicted therapeutic concentrations in the kidney, urine osmolality after administration of 1-deamino-8-D-arginine-vasopressin was approximately 700 mosm/kg H2O lower in UTBinh-14–treated mice than vehicle-treated mice. UTBinh-14 also increased urine output and reduced urine osmolality in mice given free access to water. UTBinh-14 did not reduce urine osmolality in UT-B knockout mice. In summary, these data provide proof of concept for the potential utility of UT inhibitors to reduce urinary concentration in high-vasopressin, fluid-retaining conditions. The diuretic mechanism of UT inhibitors may complement the action of conventional diuretics, which target sodium transport." @default.
• W2145910029 created "2016-06-24" @default.
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• W2145910029 date "2012-07-01" @default.
• W2145910029 modified "2023-09-27" @default.
• W2145910029 title "Triazolothienopyrimidine Inhibitors of Urea Transporter UT-B Reduce Urine Concentration" @default.
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• W2145910029 doi "https://doi.org/10.1681/asn.2011070751" @default.
• W2145910029 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3380644" @default.
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