ArticleThe journal of physiological sciences : JPS2012
Voltage-dependent biphasic effects of chloroquine on delayed rectifier K(+)-channel currents in murine thymocytes.
Article in The journal of physiological sciences : JPS, 2012. 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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17 citing papers in PubMed, 38 citations in OpenAlex.
- Chloroquine Causes Aging-like Changes in Diaphragm Neuromuscular Junction Morphology in Mice.Cells · 2025Article
- Pathological and functional significance of aging mouse kidneys: clinical implications to reduce the risk of hyper- or hypokalemia in the elderly.Kidney research and clinical practice · 2024Article
- Brief review on repurposed drugs and vaccines for possible treatment of COVID-19.European journal of pharmacology · 2021Review
- Statins as inhibitors of voltage-gated potassium channels Kv1.3 in cancer cells.Journal of molecular structure · 2021Article
- Optimizing Hydroxychloroquine Dosing for Patients With COVID-19: An Integrative Modeling Approach for Effective Drug Repurposing.Clinical pharmacology and therapeutics · 2020Article
- Margatoxin mitigates CCl4‑induced hepatic fibrosis in mice via macrophage polarization, cytokine secretion and STAT signaling.International journal of molecular medicine · 2020Article
- Blockage of Kv1.3 regulates macrophage migration in acute liver injury by targeting δ-catenin through RhoA signaling.International journal of biological sciences · 2020Article
- Second-Generation Histamine H1 Receptor Antagonists Suppress Delayed Rectifier KBioMed research international · 2019Article
- Delayed Rectifier KBioMed research international · 2019Article
- Nonsteroidal Anti-Inflammatory Drugs Quickly Resolve Symptoms Associated with EBV-Induced Infectious Mononucleosis in Patients with Atopic Predispositions.The American journal of case reports · 2016Article
- Lymphocyte Kv1.3-channels in the pathogenesis of chronic obstructive pulmonary disease: novel therapeutic implications of targeting the channels by commonly used drugs.Allergy, asthma, and clinical immunology : official journal of the Canadian Society of Allergy and Clinical Immunology · 2016Review
- Usefulness of targeting lymphocyte Kv1.3-channels in the treatment of respiratory diseases.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2015Article
- Roles of lymphocyte kv1.3-channels in the pathogenesis of renal diseases and novel therapeutic implications of targeting the channels.Mediators of inflammation · 2015Review
- Physiological significance of delayed rectifier K(+) channels (Kv1.3) expressed in T lymphocytes and their pathological significance in chronic kidney disease.The journal of physiological sciences : JPS · 2015Review
- A case of fitz-hugh-curtis syndrome complicated by appendicitis conservatively treated with antibiotics.Clinical medicine insights. Case reports · 2013Article
- Overexpression of Delayed Rectifier K(+) Channels Promotes In situ Proliferation of Leukocytes in Rat Kidneys with Advanced Chronic Renal Failure.International journal of nephrology · 2012Article
- Compensatory thrombopoietin production from the liver and bone marrow stimulates thrombopoiesis of living rat megakaryocytes in chronic renal failure.Nephron extra · 2011Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Lymphocytes are of rich in delayed rectifier K(+)-channels (Kv1.3) in their plasma membranes, and the channels play crucial roles in the lymphocyte activation and proliferation. Since chloroquine, a widely used anti-malarial drug, exerts immunosuppressive effects, it will affect the channel currents in lymphocytes. In the present study, employing the standard patch-clamp whole-cell recording technique, we examined the effects of chloroquine on the channels expressed in murine thymocytes. Published papers report that chloroquine will inhibit voltage-dependent K(+)-channel currents by plugging into the open-pore. We observed, indeed, that chloroquine suppressed the pulse-end currents of Kv1.3-channels at higher voltage steps. Surprisingly, however, we found that the drug enhanced the peak currents at both higher and lower voltage steps. Since chloroquine showed such biphasic effects on the thymocyte K(+)-channels, and since those effects were voltage dependent, we examined the effects of chloroquine on the activation and the inactivation of the channel currents. We noted that chloroquine shifted both the activation and the inactivation curves toward the hyperpolarizing potential, and that those shifts were more emphasized at lower voltage steps. We conclude that chloroquine facilitates both the activation and the inactivation of Kv1.3-channel currents in thymocytes, and that those effects are voltage dependent.
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