Effects of linalool on [(3)H]MK801 and [(3)H] muscimol binding in mouse cortical membranes

Phytother Res. 2001 Aug;15(5):422-5. doi: 10.1002/ptr.973.


Linalool is a monoterpene compound reported to be a major component of essential oils of several aromatic species. Several linalool-producing species are used in traditional medical systems for sedative purposes, including the interruption and prevention of seizures. Previous studies in mice revealed that linalool modulates glutamatergic (competitive antagonism of L-[(3)H]glutamate binding, delayed intraperitoneal NMDA-induced convulsions and blockade of intracerebroventricular Quin-induced convulsions) and GABAergic transmission (protection against pentylenetetrazol and picrotoxin-induced convulsions). To further clarify the anticonvulsive mechanisms of linalool, we studied the effects of linalool on binding of [(3)H]MK801 (NMDA antagonist) and [(3)H]muscimol (GABA(A) agonist) to mouse cortical membranes. Linalool showed a dose dependent non-competitive inhibition of [(3)H]MK801 binding (IC(50) = 2.97 mM) but no effect on [(3)H]muscimol binding. The data suggest that the anticonvulsant mode of action of linalool includes a direct interaction with the NMDA receptor complex. The data do not, however, support a direct interaction of linalool with GABA(A) receptors, although changes in GABA-mediated neuronal inhibition or effects on GABA release and uptake cannot be ruled out.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acyclic Monoterpenes
  • Animals
  • Anticonvulsants / pharmacology*
  • Brain / drug effects*
  • Dizocilpine Maleate / pharmacokinetics*
  • GABA Agonists / pharmacokinetics*
  • Male
  • Mice
  • Monoterpenes*
  • Muscimol / pharmacokinetics*
  • Plant Oils / pharmacology
  • Plants, Medicinal*
  • Receptors, N-Methyl-D-Aspartate / agonists*
  • Terpenes / pharmacology*
  • Tritium


  • Acyclic Monoterpenes
  • Anticonvulsants
  • GABA Agonists
  • Monoterpenes
  • Plant Oils
  • Receptors, N-Methyl-D-Aspartate
  • Terpenes
  • Tritium
  • Muscimol
  • Dizocilpine Maleate
  • linalool