ArticleActa pharmacologica Sinica2020
A thienopyridine, CB-20, exerts diuretic activity by inhibiting urea transporters.
Article in Acta pharmacologica Sinica, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 21 citations in OpenAlex.
- Urea, TMAO, betaine and other osmolytes as endogenous diuretics in heart failure and hypertension.Heart failure reviews · 2025Review
- Ammonia transport mediated by urea transporter A isoforms.Biology open · 2025Article
- Druggability Studies of Benzene Sulfonamide Substituted Diarylamide (E3) as a Novel Diuretic.Biomedicines · 2025Article
- Identification and Validation of Urea Transporter B Inhibitor fromMolecules (Basel, Switzerland) · 2025Article
- Small-Molecule Inhibitors and Drug Discovery of Urea Transporters.Sub-cellular biochemistry · 2025Review
- Structural characterization of human urea transporters UT-A and UT-B and their inhibition.Science advances · 2023Article
- A critical analysis of urea transporter B inhibitors: molecular fingerprints, pharmacophore features for the development of next-generation diuretics.Molecular diversity · 2022Article
- Preclinical Pharmacokinetic Studies of a Novel Diuretic Inhibiting Urea Transporters.Molecules (Basel, Switzerland) · 2022Article
- The Diuretic Effects of Coconut Water by Suppressing Aquaporin and Renin-Angiotensin-Aldosterone System in Saline-Loaded Rats.Frontiers in nutrition · 2022Article
- Discovery of novel diarylamides as orally active diuretics targeting urea transporters.Acta pharmaceutica Sinica. B · 2021Article
- The urea transporter UT-A1 plays a predominant role in a urea-dependent urine-concentrating mechanism.The Journal of biological chemistry · 2020Article
- Urea-aromatic interactions in biology.Biophysical reviews · 2020Review
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Urea transporters (UTs) are transmembrane proteins selectively permeable to urea and play an important role in urine concentration. UT-knockout mice exhibit the urea-selective urine-concentrating defect, without affecting electrolyte balance, suggesting that UT-B inhibitors have the potential to be developed as novel diuretics. In this study, we characterized a novel compound 5-ethyl-2-methyl-3-amino-6-methylthieno[2,3-b]pyridine-2,5-dicarboxylate (CB-20) with UT inhibitory activity as novel diuretics with excellent pharmacological properties. This compound was discovered based on high-throughput virtual screening combined with the erythrocyte osmotic lysis assay. Selectivity of UT inhibitors was assayed using transwell chambers. Diuretic activity of the compound was examined in rats and mice using metabolic cages. Pharmacokinetic parameters were detected in rats using LC-MS/MS. Molecular docking was employed to predict the potential binding modes for the CB-20 with human UT-B. This compound dose-dependently inhibited UT-facilitated urea transport with IC
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