ArticleThe Journal of membrane biology2008
Block of persistent late Na+ currents by antidepressant sertraline and paroxetine.
Article in The Journal of membrane biology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 39 citations in OpenAlex.
- A Thorough QT Study to Evaluate the Effects of a Supratherapeutic Dose of Sertraline on Cardiac Repolarization in Healthy Subjects.Clinical pharmacology in drug development · 2020Trial
- A case report on the safety and efficacy of aripiprazole for depression in Brugada syndrome.The mental health clinician · 2025Article
- The Antidepressant Paroxetine Reduces the Cardiac Sodium Current.International journal of molecular sciences · 2023Article
- Sertraline induces DNA damage and cellular toxicity in Drosophila that can be ameliorated by antioxidants.Scientific reports · 2020Article
- Post-SSRI Sexual Dysfunction: A Bioelectric Mechanism?Bioelectricity · 2020Article
- Post-SSRI sexual dysfunction & other enduring sexual dysfunctions.Epidemiology and psychiatric sciences · 2019Article
- Review
- Clinical Utility Gene Card for: autosomal dominant myotonia congenita (Thomsen Disease).European journal of human genetics : EJHG · 2018Article
- Antidepressant drug paroxetine blocks the open pore of Kv3.1 potassium channel.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2018Article
- Sertraline Induces Toxicity and Behavioral Alterations in Planarians.BioMed research international · 2017Article
- Selective serotonin reuptake inhibitor sertraline inhibits voltage-dependent K+ channels in rabbit coronary arterial smooth muscle cells.Journal of biosciences · 2016Article
- Blockade of Kv1.5 channels by the antidepressant drug sertraline.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2016Article
- Blockade of Kv1.5 by paroxetine, an antidepressant drug.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2016Article
- Inhibition of autophagy suppresses sertraline-mediated primary ciliogenesis in retinal pigment epithelium cells.PloS one · 2015Article
- Antidepressant therapy in epilepsy: can treating the comorbidities affect the underlying disorder?British journal of pharmacology · 2013Review
- Wide spectrum of inhibitory effects of sertraline on cardiac ion channels.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2012Article
- Interaction of morphine and selective serotonin receptor inhibitors in rats experiencing inflammatory pain.Journal of Korean medical science · 2012Article
- Sertraline inhibits formalin-induced nociception and cardiovascular responses.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologica · 2012Article
- The non-dystrophic myotonias: molecular pathogenesis, diagnosis and treatment.Brain : a journal of neurology · 2010Review
- Can a Selective Serotonin Reuptake Inhibitor Act as a Glutamatergic Modulator?Current therapeutic research, clinical and experimentalArticle
Corrections and comments
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Authors and funding
3 authors at 3 institutions in 1 country.
Funding
Abstract
Antidepressants, such as traditional tricyclic antidepressants (TCAs), are the first-line treatment for various pain syndromes. Available evidence indicates that TCAs may target Na+ channels for their analgesic action. In this report, we examined the effects of contemporary antidepressants sertraline and paroxetine on (1) neuronal Na+ channels expressed in GH3 cells and (2) muscle rNav1.4 Na+ channels heterologously expressed in Hek293t cells. Our results showed that both antidepressants blocked Na+ channels in a highly state-dependent manner. The 50% inhibitory concentrations (IC50) for sertraline and paroxetine ranged approximately 18-28 microM: for resting block and approximately 2-8 microM: for inactivated block of neuronal and rNav1.4 Na+ channels. Surprisingly, the IC50 values for both drugs were about 0.6-0.7 microM: for the open channel block of persistent late Na+ currents generated through inactivation-deficient rNav1.4 mutant Na+ channels. For comparison, the open channel block in neuronal hNav1.7 counterparts yielded IC50 values around 0.3-0.4 microM: for both drugs. Receptor mapping using fast inactivation-deficient rNav1.4-F1579A/K mutants with reduced affinities toward local anesthetics (LAs) and TCAs indicated that the F1579 residue is not involved in the binding of sertraline and paroxetine. Thus, sertraline and paroxetine are potent open channel blockers that target persistent late Na+ currents preferentially, but their block is not mediated via the phenylalanine residue at the known LA/TCA receptor site.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.