ArticleBritish journal of pharmacology2001
Phloretin differentially inhibits volume-sensitive and cyclic AMP-activated, but not Ca-activated, Cl(-) channels.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed, 80 citations in OpenAlex.
- LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial.Clinical pharmacology and therapeutics · 2012Trial
- Binding to Albumin and Off-Target Toxicity Confound the Use of LRRC8/VRAC Channel Blockers in Cell Physiology Assays.bioRxiv : the preprint server for biology · 2026Article
- Mechanism of action of two potent LRRC8/VRAC channel inhibitors.Research square · 2026Article
- Physiology of the volume-sensitive/regulatory anion channel VSOR/VRAC. Part 1: from its discovery and phenotype characterization to the molecular entity identification.The journal of physiological sciences : JPS · 2024Review
- A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC).Channels (Austin, Tex.) · 2022Review
- Effect of AQP Inhibition on Boar Sperm Cryotolerance Depends on the Intrinsic Freezability of the Ejaculate.International journal of molecular sciences · 2019Article
- Aquaglyceroporins but not orthodox aquaporins are involved in the cryotolerance of pig spermatozoa.Journal of animal science and biotechnology · 2019Article
- Brain Transport Profiles of Ginsenoside RbFrontiers in pharmacology · 2018Article
- Distinct pharmacological and molecular properties of the acid-sensitive outwardly rectifying (ASOR) anion channel from those of the volume-sensitive outwardly rectifying (VSOR) anion channel.Pflugers Archiv : European journal of physiology · 2016Article
- Volume-regulated anion channel--a frenemy within the brain.Pflugers Archiv : European journal of physiology · 2016Review
- Biophysics and Physiology of the Volume-Regulated Anion Channel (VRAC)/Volume-Sensitive Outwardly Rectifying Anion Channel (VSOR).Pflugers Archiv : European journal of physiology · 2016Review
- Structure of urea transporters.Sub-cellular biochemistry · 2014Review
- Article
- Facilitated uptake of a bioactive metabolite of maritime pine bark extract (pycnogenol) into human erythrocytes.PloS one · 2013Article
- Volume-sensitive anion channels mediate osmosensitive glutathione release from rat thymocytes.PloS one · 2013Article
- Domain-based biosensor assay to screen for epidermal growth factor receptor modulators in live cells.Assay and drug development technologies · 2012Article
- The apoptotic volume decrease is an upstream event of MAP kinase activation during Staurosporine-induced apoptosis in HeLa cells.International journal of molecular sciences · 2012Article
- Nonsynaptic communication through ATP release from volume-activated anion channels in axons.Science signaling · 2010Article
- Aquaporin biology and nervous system.Current neuropharmacology · 2010Article
- Bradykinin-induced astrocyte-neuron signalling: glutamate release is mediated by ROS-activated volume-sensitive outwardly rectifying anion channels.The Journal of physiology · 2009Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Some phenol derivatives are known to block volume-sensitive Cl(-) channels. However, effects on the channel of the bisphenol phloretin, which is a known blocker of glucose uniport and anion antiport, have not been examined. In the present study, we investigated the effects of phloretin on volume-sensitive Cl(-) channels in comparison with cyclic AMP-activated CFTR Cl(-) channels and Ca(2+)-activated Cl(-) channels using the whole-cell patch-clamp technique. Extracellular application of phloretin (over 10 microM) voltage-independently, and in a concentration-dependent manner (IC(50) approximately 30 microM), inhibited the Cl(-) current activated by a hypotonic challenge in human epithelial T84, Intestine 407 cells and mouse mammary C127/CFTR cells. In contrast, at 30 microM phloretin failed to inhibit cyclic AMP-activated Cl(-) currents in T84 and C127/CFTR cells. Higher concentrations (over 100 microM) of phloretin, however, partially inhibited the CFTR Cl(-) currents in a voltage-dependent manner. At 30 and 300 microM, phloretin showed no inhibitory effect on Ca(2+)-dependent Cl(-) currents induced by ionomycin in T84 cells. It is concluded that phloretin preferentially blocks volume-sensitive Cl(-) channels at low concentrations (below 100 microM) and also inhibits cyclic AMP-activated Cl(-) channels at higher concentrations, whereas phloretin does not inhibit Ca(2+)-activated Cl(-) channels in epithelial cells.
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