ArticleActa pharmacologica Sinica2015
Inhibition of Nav1.7 channels by methyl eugenol as a mechanism underlying its antinociceptive and anesthetic actions.
Article in Acta pharmacologica Sinica, 2015. 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, 49 citations in OpenAlex.
- Methyl eugenol increases neural microcirculation to promote nerve repair by regulating endothelial cell and Schwann cell communication via Ptn/Sdc4.Natural products and bioprospecting · 2026Article
- Phytochemical-based therapeutics from traditional eastern medicine: analgesic effects and ion channel modulation.Frontiers in pain research (Lausanne, Switzerland) · 2025Review
- Eugenol and lidocaine inhibit voltage-gated NaFrontiers in pharmacology · 2024Article
- The effect of eugenol anesthesia on the electric organ discharge of the weakly electric fish Apteronotus leptorhynchus.Fish physiology and biochemistry · 2023Article
- Plant and fungi derived analgesic natural products targeting voltage-gated sodium and calcium channels.Channels (Austin, Tex.) · 2022Review
- Non-Volatile and Volatile Bioactives ofAntioxidants (Basel, Switzerland) · 2022Article
- Possible Use of Phytochemicals for Recovery from COVID-19-Induced Anosmia and Ageusia.International journal of molecular sciences · 2021Review
- Measurement of CORSC advances · 2021Article
- Co-Application of Eugenol and QX-314 Elicits the Prolonged Blockade of Voltage-Gated Sodium Channels in Nociceptive Trigeminal Ganglion Neurons.Biomolecules · 2020Article
- Antinociceptive Interaction and Pharmacokinetics of the Combination Treatments of Methyleugenol Plus Diclofenac or Ketorolac.Molecules (Basel, Switzerland) · 2020Article
- Procaine penicillin alters swimming behaviour and physiological parameters of Daphnia magna.Environmental science and pollution research international · 2019Article
- Recent development in antihyperalgesic effect of phytochemicals: anti-inflammatory and neuro-modulatory actions.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2018Review
- Inhibitory effects of eugenol on putative nociceptive response in spinal cord preparation isolated from neonatal rats.Experimental brain research · 2018Article
- Essential Oils and Their Constituents Targeting the GABAergic System and Sodium Channels as Treatment of Neurological Diseases.Molecules (Basel, Switzerland) · 2018Review
- Analgesic-Like Activity of Essential Oil Constituents: An Update.International journal of molecular sciences · 2017Review
- Pain transduction: a pharmacologic perspective.Expert review of clinical pharmacology · 2016Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
aimMethyl eugenol is a major active component extracted from the Chinese herb Asari Radix et Rhizoma, which has been used to treat toothache and other pain. Previous in vivo studies have shown that methyl eugenol has anesthetic and antinociceptive effects. The aim of this study was to determine the possible mechanism underlying its effect on nervous system disorders.
methodsThe direct interaction of methyl eugenol with Na(+) channels was explored and characterized using electrophysiological recordings from Nav1.7-transfected CHO cells.
resultsIn whole-cell patch clamp mode, methyl eugenol tonically inhibited peripheral nerve Nav1.7 currents in a concentration- and voltage-dependent manner, with an IC50 of 295 μmol/L at a -100 mV holding potential. Functionally, methyl eugenol preferentially bound to Nav1.7 channels in the inactivated and/or open state, with weaker binding to channels in the resting state. Thus, in the presence of methyl eugenol, Nav1.7 channels exhibited reduced availability for activation in a steady-state inactivation protocol, strong use-dependent inhibition, enhanced binding kinetics, and slow recovery from inactivation compared to untreated channels. An estimation of the affinity of methyl eugenol for the resting and inactivated states of the channel also demonstrated that methyl eugenol preferentially binds to inactivated channels, with a 6.4 times greater affinity compared to channels in the resting state. The failure of inactivated channels to completely recover to control levels at higher concentrations of methyl eugenol implies that the drug may drive more drug-bound, fast-inactivated channels into drug-bound, slow-inactivated channels.
conclusionMethyl eugenol is a potential candidate as an effective local anesthetic and analgesic. The antinociceptive and anesthetic effects of methyl eugenol result from the inhibitory action of methyl eugenol on peripheral Na(+) channels.
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