ArticleThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology2016
Blockade of Kv1.5 channels by the antidepressant drug sertraline.
Article in The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 20 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
- Neonatal Clomipramine Exposure Disrupts Epididymal Serotonin Signaling and Programs Sperm Dysfunction in Adult Rats.International journal of molecular sciences · 2026Article
- The involvement of KTranslational psychiatry · 2024Review
- Effects of rosiglitazone, an antidiabetic drug, on Kv3.1 channels.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2023Article
- The antidiabetic drug rosiglitazone blocks Kv1.5 potassium channels in an open state.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2022Article
- Open channel block of Kv1.5 channels by HMQ1611.Frontiers in pharmacology · 2022Article
- The antidepressant Sertraline inhibits CatSper Ca2+ channels in human sperm.Human reproduction (Oxford, England) · 2021Article
- Open channel block of Kv1.4 potassium channels by aripiprazole.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2020Article
- Post-SSRI Sexual Dysfunction: A Bioelectric Mechanism?Bioelectricity · 2020Article
- Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5.Biomolecules · 2019Review
- Escitalopram, a selective serotonin reuptake inhibitor, inhibits voltage-dependent KThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2017Article
- Nortriptyline, a tricyclic antidepressant, inhibits voltage-dependent KThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2017Article
- Inhibitory effects of cholinesterase inhibitor donepezil on the Kv1.5 potassium channel.Scientific reports · 2017Article
- Sertraline Induces Toxicity and Behavioral Alterations in Planarians.BioMed research international · 2017Article
- Facilitation of serotonin-induced contraction of rat mesenteric artery by ketamine.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2016Article
- Can a Selective Serotonin Reuptake Inhibitor Act as a Glutamatergic Modulator?Current therapeutic research, clinical and experimentalArticle
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Sertraline, a selective serotonin reuptake inhibitor (SSRI), has been reported to lead to cardiac toxicity even at therapeutic doses including sudden cardiac death and ventricular arrhythmia. And in a SSRI-independent manner, sertraline has been known to inhibit various voltage-dependent channels, which play an important role in regulation of cardiovascular system. In the present study, we investigated the action of sertraline on Kv1.5, which is one of cardiac ion channels. The eff ect of sertraline on the cloned neuronal rat Kv1.5 channels stably expressed in Chinese hamster ovary cells was investigated using the whole-cell patch-clamp technique. Sertraline reduced Kv1.5 whole-cell currents in a reversible concentration-dependent manner, with an IC 50 value and a Hill coefficient of 0.71 µM and 1.29, respectively. Sertraline accelerated the decay rate of inactivation of Kv1.5 currents without modifying the kinetics of current activation. The inhibition increased steeply between -20 and 0 mV, which corresponded with the voltage range for channel opening. In the voltage range positive to +10 mV, inhibition displayed a weak voltage dependence, consistent with an electrical distance δ of 0.16. Sertraline slowed the deactivation time course, resulting in a tail crossover phenomenon when the tail currents, recorded in the presence and absence of sertraline, were superimposed. Inhibition of Kv1.5 by sertraline was use-dependent. The present results suggest that sertraline acts on Kv1.5 currents as an open-channel blocker.
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