19 Harley St, London, W1G 9QJ, UK

Menthol pain relief through cumulative inactivation of voltage-gated sodium channels

Menthol is a natural compound of plant origin known to produce cool sensation via the activation of the TRPM8 channel. It is also frequently part of topical analgesic drugs available in a pharmacy, although its mechanism of action is still unknown. Compelling evidence indicates that voltage-gated Na(+) channels are critical for experiencing pain sensation. We tested the hypothesis that menthol may block voltage-gated Na(+) channels in dorsal root ganglion (DRG) neurons. By use of a patch clamp, we evaluated the effects of menthol application on tetrodotoxin (TTX)-resistant Nav1.8 and Nav1.9 channel subtypes in DRG neurons, and on TTX-sensitive Na(+) channels in immortalized DRG neuron-derived F11 cells. The results indicate that menthol inhibits Na(+) channels in a concentration-, voltage-, and frequency-dependent manner. Menthol promoted fast and slow inactivation states, causing use-dependent depression of Na(+) channel activity. In current clamp recordings, menthol inhibited firing at high-frequency stimulation with minimal effects on normal neuronal activity. We found that low concentrations of menthol cause analgesia in mice, relieving pain produced by a Na(+) channel-targeting toxin. We conclude that menthol is a state-selective blocker of Nav1.8, Nav1.9, and TTX-sensitive Na(+) channels, indicating a role for Na(+) channel blockade in the efficacy of menthol as topical analgesic compound

Keywords : Analgesia,Analgesics,Animals,Cell Line,Tumor,Depression,drug therapy,France,Hybrid Cells,Male,Menthol,metabolism,Mice,Mice,Inbred C57BL,NAV1.8 Voltage-Gated Sodium Channel,NAV1.9 Voltage-Gated Sodium Channel,Neural Inhibition,Neuroblastoma,Neurons,Pain,pharmacology,physiology,physiopathology,Primary Cell Culture,Rats,Rats,Wistar,Sensation,Sodium,Sodium Channels,Tetrodotoxin,, Pain,Relief,Through,Cumulative,Inactivation, pars defect treatment

Date of Publication : 2012 Feb

Authors : Gaudioso C;Hao J;Martin-Eauclaire MF;Gabriac M;Delmas P;

Organisation : Centre de Recherche en Neurobiologie et Neurophysiologie de Marseille, Aix-Marseille Universite, UMR 6231, CNRS, CS80011, Bd Pierre Dramard, 13344 Marseille Cedex 15, France. christelle.gaudioso@univmed.fr

Journal of Publication : Pain

Pubmed Link : https://www.ncbi.nlm.nih.gov/pubmed/22172548

The London Spine Unit : Harley Street UK. Specialists in Cutting Edge Technologies for Spinal Surgery

Make an Appointment 

Trustpilot Reviews
Doctify Reviews
Top Doctor Reviews

Menthol pain relief through cumulative inactivation of voltage-gated sodium channels | Mri scans london

What our patients say ...

Consultant Spine Surgeon
Consultant Spine Surgeon
Consultant Spine Surgeon

This surgical technique consists of a percutaneous approach for the treatment of small to medium size hernias of the intervertebral disc by laser energy. The main objective is to reduce the intradiscal pressure in the nucleus pulposus

Laser Disc Surgery can be performed under local anaesthetic as a day case at our centre on the prestigious Harley Street.
What is London spine unit and How it Works

The London Spine Unit was established in 2005 and has successfully treated over 5000 patients. All conditions are treated.

treatment of all spinal disorders

The London Spine Unit specialises in Minimally Invasive Treatments allowing rapid recovery and return to normal function

Trusted by patients worldwide

The London Spine Unit provides the highest quality care to all patients and has VIP services for those seeking exceptional services

If you have any emergency Doctor’s need, simply call our 24 hour emergency

Your personal case manager will ensure that you receive the best possible care.

Call Now 

+44 844 589 2020
+44 203 973 8810