Linalool modifies the nicotinic receptor-ion channel kinetics at the mouse neuromuscular junction

Pharmacol Res. 2000 Aug;42(2):177-82. doi: 10.1006/phrs.2000.0671.


Linalool is a monoterpene compound reported to be a major component of essential oils in various aromatic species. Several linalool-producing species are used in traditional medical systems. Among these is Aeolanthus suaveolens G. Dom (Labiatae) which is used as an anticonvulsant in the Brazilian Amazon. Psychopharmacological in vivo evaluation of linalool showed that this compound has dose-dependent marked sedative effects at the central nervous system (CNS), including hypnotic, anticonvulsant and hypothermic properties. It has been suggested that these neurochemical effects might be ascribed to the local anaesthetic activity of linalool. The present study reports an inhibitory effect of linalool on the acetylcholine (ACh) release and on the channel open time in the mouse neuromuscular junction. These findings could provide a rational basis to confirm the traditional medical use of linalool-producing plant species. Indeed, our data demonstrate some interactions in the modulation of the ACh release at the mouse neuromuscular junction, which are well correlated with the suggested molecular mechanisms. Linalool induced a reduction of the ACh-evoked release. The possibility that this effect could be ascribed to some interaction with pre-synaptic function is noteworthy. Moreover, the inhibitory effect induced on the kinetics of the miniature end-plate current decay demonstrates a local anaesthetic action, either on the voltage or on the receptor-activated channels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholine / metabolism
  • Acyclic Monoterpenes
  • Animals
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Ion Channel Gating / drug effects
  • Ion Channels / drug effects
  • Kinetics
  • Male
  • Membrane Potentials / drug effects
  • Mice
  • Monoterpenes*
  • Motor Endplate / drug effects
  • Motor Endplate / physiology
  • Neuromuscular Junction / drug effects*
  • Neuromuscular Junction / metabolism
  • Nicotinic Antagonists / pharmacology
  • Patch-Clamp Techniques
  • Receptors, Nicotinic / physiology*
  • Terpenes / pharmacology*


  • Acyclic Monoterpenes
  • Ion Channels
  • Monoterpenes
  • Nicotinic Antagonists
  • Receptors, Nicotinic
  • Terpenes
  • linalool
  • Acetylcholine