ArticleBritish journal of pharmacology1999
Block by fluoxetine of volume-regulated anion channels.
Article in British journal of pharmacology, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 65 citations in OpenAlex.
- Mechanosensing in Metabolism.Comprehensive Physiology · 2023Review
- Pharmacological modulation of chloride channels as a therapeutic strategy for neurological disorders.Frontiers in physiology · 2023Review
- Molecular logic of salt taste reception in special reference to transmembrane channel-like 4 (TMC4).The journal of physiological sciences : JPS · 2022Review
- VI-116, A Novel Potent Inhibitor of VRAC with Minimal Effect on ANO1.International journal of molecular sciences · 2022Article
- The Fight against COVID-19 on the Multi-Protease Front and Surroundings: Could an Early Therapeutic Approach with Repositioning Drugs Prevent the Disease Severity?Biomedicines · 2021Review
- Article
- Biophysics and Physiology of the Volume-Regulated Anion Channel (VRAC)/Volume-Sensitive Outwardly Rectifying Anion Channel (VSOR).Pflugers Archiv : European journal of physiology · 2016Review
- Selective serotonin reuptake inhibitors facilitate ANO6 (TMEM16F) current activation and phosphatidylserine exposure.Pflugers Archiv : European journal of physiology · 2015Article
- Article
- The GABAergic deficit hypothesis of major depressive disorder.Molecular psychiatry · 2011Article
- Inhibition of G protein-activated inwardly rectifying K+ channels by different classes of antidepressants.PloS one · 2011Article
- Influenza A virus inhibits alveolar fluid clearance in BALB/c mice.American journal of respiratory and critical care medicine · 2008Article
- Inhibition of G protein-activated inwardly rectifying K+ channels by fluoxetine (Prozac).British journal of pharmacology · 2003Article
- Volume-regulated anion channels serve as an auto/paracrine nucleotide release pathway in aortic endothelial cells.The Journal of general physiology · 2002Article
- Chlorotoxin does not inhibit volume-regulated, calcium-activated and cyclic AMP-activated chloride channels.British journal of pharmacology · 2000Article
- Inhibition of neuronal KV potassium currents by the antidepressant drug, fluoxetine.British journal of pharmacology · 1999Article
- Development and validation of fluorescence-based and automated patch clamp-based functional assays for the inward rectifier potassium channel Kir4.1.Assay and drug development technologiesArticle
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. We have used the whole-cell patch clamp technique to study the effect of fluoxetine, a commonly used antidepressant drug, on the volume-regulated anion channel (VRAC) in calf pulmonary artery endothelial (CPAE) cells. We also examined its effects on other Cl- channels, i.e. the Ca2(+)-activated Cl- current (I(Cl,Ca) and the cystic fibrosis transmembrane conductance regulator (CFTR) to assess the specificity of this compound for VRAC. 2. At pH 7.4 fluoxetine induced a fast and reversible block of the volume-sensitive chloride current (I(Cl,swell)), with a Ki value of 6.0+/-0.5 microM (n = 6-9). The blocking efficiency increased with increasing extracellular pH (Ki= 0.32+/-0.01 microM at pH 8.8, n = 3-9), indicating that the blockade is mediated by the uncharged form of fluoxetine. 3. Fluoxetine inhibited Ca2(+)-activated Cl(-) currents, I(Cl,Ca), activated by loading CPAE cells via the patch pipette with 1000 nM free Ca2+ (Ki= 10.7+/-1.6 microm at pH 7.4, n=3-5). The CFTR channel, transiently transfected in CPAE cells, was also inhibited with a Ki value of 26.9+/-9.4 microM at pH 7.4 (n = 3). 4. This study describes for the first time the effects of fluoxetine on anion channels. Our data reveal a potent block of VRAC at fluoxetine concentrations close to plasma concentrations. The results suggest a hydrophobic interaction with high affinity between uncharged fluoxetine and volume-activated chloride channels. Ca(2+)-activated Cl- currents and CFTR are also blocked by fluoxetine, revealing a novel characteristic of the drug as a chloride channel modulator.
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