ArticleCNS neuroscience & therapeutics2015
Local anesthetic lidocaine inhibits TRPM7 current and TRPM7-mediated zinc toxicity.
Article in CNS neuroscience & therapeutics, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 33 citations in OpenAlex.
- Anesthetics in pathological cerebrovascular conditions.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2025Review
- Role of Cholesterol Metabolic Enzyme CYP46A1 and Its Metabolite 24S-Hydroxycholesterol in Ischemic Stroke.Stroke · 2024Article
- The role of lidocaine in cancer progression and patient survival.Pharmacology & therapeutics · 2024Review
- Cell death induction and protection by activation of ubiquitously expressed anion/cation channels. Part 3: the roles and properties of TRPM2 and TRPM7.Frontiers in cell and developmental biology · 2023Review
- Review
- Upregulation of acid sensing ion channel 1a (ASIC1a) by hydrogen peroxide through the JNK pathway.Acta pharmacologica Sinica · 2021Article
- Article
- Perioperative Intravenous Lidocaine and Metastatic Cancer Recurrence - A Narrative Review.Frontiers in oncology · 2021Review
- Protein Kinase C Regulates ASIC1a Protein Expression and Channel Function via NF-kB Signaling Pathway.Molecular neurobiology · 2020Article
- Role of the chanzyme TRPM7 in the nervous system in health and disease.Cellular and molecular life sciences : CMLS · 2019Review
- Acute Ethanol Exposure Promotes Autophagy-Lysosome Pathway-Dependent ASIC1a Protein Degradation and Protects Against Acidosis-Induced Neurotoxicity.Molecular neurobiology · 2019Article
- TRPM7 channels play a role in high glucose-induced endoplasmic reticulum stress and neuronal cell apoptosis.The Journal of biological chemistry · 2018Article
- Effect of Redox-Modifying Agents on the Activity of Channelrhodopsin-2.CNS neuroscience & therapeutics · 2017Article
- TRPM7 is a unique target for therapeutic intervention of stroke.International journal of physiology, pathophysiology and pharmacology · 2017Review
- Lidocaine suppresses glioma cell proliferation by inhibiting TRPM7 channels.International journal of physiology, pathophysiology and pharmacology · 2017Article
- Serum- and glucocorticoid-inducible kinases in microglia.Biochemical and biophysical research communications · 2016Article
- Amiloride Analogs as ASIC1a Inhibitors.CNS neuroscience & therapeutics · 2016Article
- Lidocaine Inhibits HCN Currents in Rat Spinal Substantia Gelatinosa Neurons.Anesthesia and analgesia · 2016Article
- Neuroprotective effect of lidocaine: is there clinical potential?International journal of physiology, pathophysiology and pharmacology · 2016Review
- Characterization of a Synthetic Steroid 24-keto-cholest-5-en-3β, 19-diol as a Neuroprotectant.CNS neuroscience & therapeutics · 2015Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
backgroundPrevious study demonstrated that overstimulation of TRPM7 substantially contributes to zinc-mediated neuronal toxicity. Inhibition of TRPM7 activity and TRPM7-mediated intracellular Zn(2+) accumulation may represent a promising strategy in the treatment of stroke.
aimsTo investigate whether local anesthetics lidocaine could inhibit TRPM7 channel and TRPM7-mediated zinc toxicity.
methodsWhole-cell patch-clamp technique was used to investigate the effect of local anesthetics on TRPM7 currents in cultured mouse cortical neurons and TRPM7-overexpressed HEK293 cells. Fluorescent Zn(2+) imaging technique was used to study the effect of lidocaine on TRPM7-mediated intracellular Zn(2+) accumulation. TRPM7-mediated zinc toxicity in neurons was used to evaluate the neuroprotective effect of lidocaine.
results(1) Lidocaine dose dependently inhibits TRPM7-like currents, with an IC50 of 11.55 and 11.06 mM in cultured mouse cortical neurons and TRPM7-overexpressed HEK293 cells, respectively; (2) Lidocaine inhibits TRPM7 currents in a use/frequency-dependent manner; (3) Lidocaine inhibits TRPM7-mediated intracellular Zn(2+) accumulation in both cortical neurons and TRPM7-overexpressed HEK293 cells; (4) TRPM7-mediated Zn(2+) toxicity is ameliorated by lidocaine in cortical neurons; (5) QX-314 has a similar inhibitory effect as lidocaine on TRPM7 currents when applied extracellularly; (6) Procaine also shows potent inhibitory effect on the TRPM7 currents in cortical neurons.
conclusionOur data provide the first evidence that local anesthetic lidocaine inhibits TRPM7 channel and TRPM7-mediated zinc toxicity.
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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.