ArticleMolecular brain2010
The modulation of TRPM7 currents by nafamostat mesilate depends directly upon extracellular concentrations of divalent cations.
Article in Molecular brain, 2010. 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, 35 citations in OpenAlex.
- Roles of TRPM channels in glioma.Cancer biology & therapy · 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
- TRPM7 is an essential regulator for volume-sensitive outwardly rectifying anion channel.Communications biology · 2021Article
- The Role of TRP Channels and PMCA in Brain Disorders: Intracellular Calcium and pH Homeostasis.Frontiers in cell and developmental biology · 2021Review
- Nafamostat mesylate attenuates the pathophysiologic sequelae of neurovascular ischemia.Neural regeneration research · 2020Review
- Mapping TRPM7 Function by NS8593.International journal of molecular sciences · 2020Review
- Nafamostat Mesilate Improves Neurological Outcome and Axonal Regeneration after Stroke in Rats.Molecular neurobiology · 2017Article
- Role of TRPM7 in Cancer: Potential as Molecular Biomarker and Therapeutic Target.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Role of transient receptor potential melastatin type 7 channel in gastric cancer.Integrative medicine research · 2016Review
- Review
- The Pathophysiologic Roles of TRPM7 Channel.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2014Review
- A sequential impairment of cortical astrocytes and GABAergic neurons during ischemia is improved by mGluR₁,₅ activation.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2013Article
- Sphingosine and FTY720 are potent inhibitors of the transient receptor potential melastatin 7 (TRPM7) channels.British journal of pharmacology · 2013Article
- TRPM7, the cytoskeleton and neuronal death.Channels (Austin, Tex.) · 2013Review
- Natural and synthetic modulators of SK (K(ca)2) potassium channels inhibit magnesium-dependent activity of the kinase-coupled cation channel TRPM7.British journal of pharmacology · 2012Article
- An anti-coagulation agent Futhan preferentially targets GABA(A) receptors in lungepithelia: implication in treating asthma.International journal of physiology, pathophysiology and pharmacology · 2011Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 3 countries.
Funding
Abstract
Concentrations of extracellular divalent cations (Ca2+ and Mg2+) fall substantially during intensive synaptic transmission as well as during some pathophysiological conditions such as epilepsy and brain ischemia. Here we report that a synthetic serine protease inhibitor, nafamostat mesylate (NM), and several of its analogues, block recombinant TRPM7 currents expressed in HEK293T cells in inverse relationship to the concentration of extracellular divalent cations. Lowering extracellular Ca2+ and Mg2+ also evokes a divalent-sensitive non-selective cation current that is mediated by TRPM7 expression in hippocampal neurons. In cultured hippocampal neurons, NM blocked these TRPM7-mediated currents with an apparent affinity of 27 μM, as well as the paradoxical Ca2+ influx associated with lowering extracellular Ca2+. Unexpectedly, pre-exposure to NM strongly potentiated TRPM7 currents. In the presence of physiological concentrations of extracellular divalent cations, NM activates TRPM7. The stimulating effects of NM on TRPM7 currents are also inversely related to extracellular Ca2+ and Mg2+. DAPI and HSB but not netropsin, blocked and stimulated TRPM7. In contrast, mono-cationic, the metabolites of NM, p-GBA and AN, as well as protease inhibitor leupeptin and gabexate failed to substantially modulate TRPM7. NM thus provides a molecular template for the design of putative modulators of TRPM7.
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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.