ArticlePloS one2011
Inhibition of G protein-activated inwardly rectifying K+ channels by different classes of antidepressants.
Article in PloS one, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 36 citations in OpenAlex.
- Antiseizure Effects of Mirtazapine in a Rat Model of Status Epilepticus Via Cannabinoid Receptor Modulation.Neurochemical research · 2025Article
- The involvement of KTranslational psychiatry · 2024Review
- Review
- Neuronal G protein-gated KAmerican journal of physiology. Cell physiology · 2022Review
- Chronic Cerebral Hypoperfusion-induced Dysregulations of Hyperpolarization- activated Cyclic Nucleotide-gated, KCNQ and G Protein-coupled Inwardly Rectifying Potassium Channels Correlated with Susceptibility and Unsusceptibility to Anxiety Behaviors.Current neurovascular research · 2022Article
- Review
- Anticraving therapy for alcohol use disorder: A clinical review.Neuropsychopharmacology reports · 2018Review
- Lack of relationship between plasma levels of escitalopram and QTc-interval length.European archives of psychiatry and clinical neuroscience · 2017Article
- Dual activation of neuronal G protein-gated inwardly rectifying potassium (GIRK) channels by cholesterol and alcohol.Scientific reports · 2017Article
- 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
- Variants in Ion Channel Genes Link Phenotypic Features of Bipolar Illness to Specific Neurobiological Process Domains.Molecular neuropsychiatry · 2015Review
- Alcohol modulation of G-protein-gated inwardly rectifying potassium channels: from binding to therapeutics.Frontiers in physiology · 2014Review
- New insights into the therapeutic potential of Girk channels.Trends in neurosciences · 2014Review
- Addition of amoxapine improves positive and negative symptoms in a patient with schizophrenia.Therapeutic advances in psychopharmacology · 2013Article
- Acute and subacute effects of the selective serotonin-noradrenaline reuptake inhibitor duloxetine on cardiac hERG channels.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- 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
- Article
- 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 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Various antidepressants are commonly used for the treatment of depression and several other neuropsychiatric disorders. In addition to their primary effects on serotonergic or noradrenergic neurotransmitter systems, antidepressants have been shown to interact with several receptors and ion channels. However, the molecular mechanisms that underlie the effects of antidepressants have not yet been sufficiently clarified. G protein-activated inwardly rectifying K(+) (GIRK, Kir3) channels play an important role in regulating neuronal excitability and heart rate, and GIRK channel modulation has been suggested to have therapeutic potential for several neuropsychiatric disorders and cardiac arrhythmias. In the present study, we investigated the effects of various classes of antidepressants on GIRK channels using the Xenopus oocyte expression assay. In oocytes injected with mRNA for GIRK1/GIRK2 or GIRK1/GIRK4 subunits, extracellular application of sertraline, duloxetine, and amoxapine effectively reduced GIRK currents, whereas nefazodone, venlafaxine, mianserin, and mirtazapine weakly inhibited GIRK currents even at toxic levels. The inhibitory effects were concentration-dependent, with various degrees of potency and effectiveness. Furthermore, the effects of sertraline were voltage-independent and time-independent during each voltage pulse, whereas the effects of duloxetine were voltage-dependent with weaker inhibition with negative membrane potentials and time-dependent with a gradual decrease in each voltage pulse. However, Kir2.1 channels were insensitive to all of the drugs. Moreover, the GIRK currents induced by ethanol were inhibited by sertraline but not by intracellularly applied sertraline. The present results suggest that GIRK channel inhibition may reveal a novel characteristic of the commonly used antidepressants, particularly sertraline, and contributes to some of the therapeutic effects and adverse effects.
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