ArticleThe Journal of general physiology2012
Local anesthetic inhibition of a bacterial sodium channel.
Article in The Journal of general physiology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed, 63 citations in OpenAlex.
- The chemistry of electrical signaling in sodium channels from bacteria and beyond.Cell chemical biology · 2024Review
- Article
- An α-π transition in S6 shapes the conformational cycle of the bacterial sodium channel NavAb.The Journal of general physiology · 2023Article
- Druggability of Voltage-Gated Sodium Channels-Exploring Old and New Drug Receptor Sites.Frontiers in pharmacology · 2022Review
- Molecular mechanism of the spider toxin κ-LhTx-I acting on the bacterial voltage-gated sodium channel NaChBac.Frontiers in pharmacology · 2022Article
- Cannabidiol Selectively Binds to the Voltage-Gated Sodium Channel NaBiomedicines · 2021Article
- Regulation and drug modulation of a voltage-gated sodium channel: Pivotal role of the S4-S5 linker in activation and slow inactivation.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Cannabidiol inhibits the skeletal muscle Nav1.4 by blocking its pore and by altering membrane elasticity.The Journal of general physiology · 2021Article
- The effects of tricaine mesylate on arthropods: crayfish, crab and Drosophila.Invertebrate neuroscience : IN · 2020Article
- Management of diabetic foot ulcers: a 25% lidocaine topical cream formulation design, physicochemical and microbiological assessments.European journal of hospital pharmacy : science and practice · 2020Article
- A Potential Mechanism of Sodium Channel Mediating the General Anesthesia Induced by Propofol.Frontiers in cellular neuroscience · 2020Article
- Comparison of permeation mechanisms in sodium-selective ion channels.Neuroscience letters · 2019Review
- Batrachotoxin acts as a stent to hold open homotetrameric prokaryotic voltage-gated sodium channels.The Journal of general physiology · 2019Article
- Molecular dissection of multiphase inactivation of the bacterial sodium channel NaThe Journal of general physiology · 2019Article
- Fenestrations control resting-state block of a voltage-gated sodium channel.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Inhibitory effects of cannabidiol on voltage-dependent sodium currents.The Journal of biological chemistry · 2018Article
- Article
- Propofol inhibits prokaryotic voltage-gated NaThe Journal of general physiology · 2018Article
- The voltage-gated sodium channel pore exhibits conformational flexibility during slow inactivation.The Journal of general physiology · 2018Article
- Propofol's paradox, explained.The Journal of general physiology · 2018Article
Corrections and comments
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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
Recent structural breakthroughs with the voltage-gated sodium channel from Arcobacter butzleri suggest that such bacterial channels may provide a structural platform to advance the understanding of eukaryotic sodium channel gating and pharmacology. We therefore set out to determine whether compounds known to interact with eukaryotic Na(V)s could also inhibit the bacterial channel from Bacillus halodurans and NaChBac and whether they did so through similar mechanisms as in their eukaryotic homologues. The data show that the archetypal local anesthetic (LA) lidocaine inhibits resting NaChBac channels with a dissociation constant (K(d)) of 260 µM, and channels displayed a left-shifted steady-state inactivation gating relationship in the presence of the drug. Extracellular application of QX-314 to expressed NaChBac channels had no effect on sodium current, whereas internal exposure via injection of a bolus of the quaternary derivative rapidly reduced sodium conductance, consistent with a hydrophilic cytoplasmic access pathway to an internal binding site. However, the neutral derivative benzocaine applied externally inhibited NaChBac channels, suggesting that hydrophobic pathways can also provide drug access to inhibit channels. Alternatively, ranolazine, a putative preopen state blocker of eukaryotic Na(V)s, displayed a K(d) of 60 µM and left-shifted the NaChBac activation-voltage relationship. In each case, block enhanced entry into the inactivated state of the channel, an effect that is well described by a simple kinetic scheme. The data suggest that although significant differences exist, LA block of eukaryotic Na(V)s also occurs in bacterial sodium channels and that NaChBac shares pharmacological homology to the resting state of vertebrate Na(V) homologues.
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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.