ArticleFrontiers in pharmacology2011
The sodium channel as a target for local anesthetic drugs.
Article in Frontiers in pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
59 citing papers in PubMed, 118 citations in OpenAlex.
- Preventing Postoperative Catheter-Related Bladder Discomfort (CRBD) with Bladder Irrigation Using 0.05% Lidocaine Saline Solution: Monitoring with Analgesia Nociception Index (ANI) after Transurethral Surgery.Medicina (Kaunas, Lithuania) · 2024Trial
- Lvguidingan inhibits Nav1.2 and epilepsy-associated SCN2A gain-of-function variants.Acta pharmacologica Sinica · 2026Article
- Functional and molecular diversity of human C-fibers in pain modulation.Current opinion in supportive and palliative care · 2026Review
- Effects of voltage-gated sodium channels on the median effective dose of ropivacaine in diabetic rats.Scientific reports · 2026Article
- The psychoactive cannabinoid THC inhibits peripheral nociceptors by targeting NaNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Effects of Extended-Release Liposomal Bupivacaine on Postoperative Mechanical and Thermal Hypersensitivity in C57BL/6 Mice (Mus musculus).Journal of the American Association for Laboratory Animal Science : JAALAS · 2026Article
- Dermal Concentration Versus Systemic Bioavailability of Topical Lidocaine and Tetracaine: An Exploratory Pharmacokinetic Pilot Study in Göttingen Minipigs.Pharmaceutics · 2025Article
- Efficacy of 10% lidocaine gel for injection site pain associated with treprostinil in the treatment of pulmonary hypertension: a report of four cases.JA clinical reports · 2025Article
- Extended osteoarthritis pain relief with neosaxitoxin using alginate-core polymeric microparticles.Nanoscale · 2025Article
- Defining the polycystin pharmacophore through high-throughput screening and computational biophysics.British journal of pharmacology · 2025Article
- Rational design, synthesis, and evaluation of novel polypharmacological compounds targeting NaThe Journal of biological chemistry · 2025Article
- Toxic and signaling effects of the anaesthetic lidocaine on rice cultured cells.Plant signaling & behavior · 2024Article
- The Stable Gastric Pentadecapeptide BPC 157 Pleiotropic Beneficial Activity and Its Possible Relations with Neurotransmitter Activity.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Article
- Allergy to Local Anesthetics is a Rarity: Review of Diagnostics and Strategies for Clinical Management.Clinical reviews in allergy & immunology · 2023Review
- An α-π transition in S6 shapes the conformational cycle of the bacterial sodium channel NavAb.The Journal of general physiology · 2023Article
- Blockers of Skeletal Muscle NaInternational journal of molecular sciences · 2023Review
- Capsaicin as an amphipathic modulator of NaChannels (Austin, Tex.) · 2022Article
- A Novel Photoswitchable Azobenzene-Containing Local Anesthetic Ethercaine with Light-Controlled Biological Activity In Vivo.International journal of molecular sciences · 2022Article
- 3D Printing Methyl Cellulose Hydrogel Wound Dressings with Parameter Exploration Via Computational Fluid Dynamics Simulation.Pharmaceutical research · 2022Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
Na channels are the source of excitatory currents for the nervous system and muscle. They are the target for a class of drugs called local anesthetics (LA), which have been used for local and regional anesthesia and for excitatory problems such as epilepsy and cardiac arrhythmia. These drugs are prototypes for new analgesic drugs. The drug-binding site has been localized to the inner pore of the channel, where drugs interact mainly with a phenylalanine in domain IV S6. Drug affinity is both voltage- and use-dependent. Voltage-dependency is the result of changes in the conformation of the inner pore during channel activation and opening, allowing high energy interaction of drugs with the phenylalanine. LA drugs also reduce the gating current of Na channels, which represents the movement of charged residues in the voltage sensors. Specifically, drug binding to phenylalanine locks the domain III S4 in its outward (activated) position, and slows recovery of the domain IV S4. Although strongly affecting gating, LA drugs almost certainly also block by steric occlusion of the pore. Molecular definition of the binding and blocking interactions may help in new drug development.
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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.