Antinociceptive and anticonvulsant effects of the monoterpene linalool oxide

Pharm Biol. 2017 Dec;55(1):63-67. doi: 10.1080/13880209.2016.1228682. Epub 2016 Sep 13.

Abstract

Context: Linalool oxide (OXL) (a monoterpene) is found in the essential oils of certain aromatic plants, or it is derived from linalool. The motivation for this work is the lack of psychopharmacological studies on this substance.

Objective: To evaluate OXL's acute toxicity, along with its anticonvulsant and antinociceptive activities in male Swiss mice.

Material and methods: OXL (50, 100 and 150 mg/kg, i.p.) was investigated for acute toxicity and in the Rota-rod test. Antinociceptive activity was evaluated by the acetic acid-induced writhing test, and by formalin testing. Anticonvulsant effects were demonstrated by testing for pentylenetetrazol (PTZ)-induced seizures and by Maximum Electroshock headset (MES) test. OXL was administered to the animals intraperitoneally 30 min before for pharmacological tests.

Results: OXL showed an LD50 of ∼721 (681-765) mg/kg. In the Rota-rod test, it was observed that OXL caused no damage to the animal's motor coordination. OXL significantly reduced (p < .001) the number of writhings. OXL also significantly decreased (p < .05, p < .01 or p < .001) paw-licking time in the two phases of the formalin test. OXL significantly reduced (p < .01 or p < .001) the duration of tonic seizures in the MES test, and at the dose 150 mg/kg, significantly increased (p < .01) the latency to first seizure in the PTZ test.

Conclusion: The tested doses of OXL were safe, with no motor impairment, and show clear antinociceptive and anticonvulsant potential. Future investigations with this monoterpene may lead to the development of a new molecule with even higher potency and selectivity.

Keywords: Pain; essential oil; nociception.

MeSH terms

  • Acetic Acid
  • Acyclic Monoterpenes
  • Analgesics / pharmacology*
  • Analgesics / toxicity
  • Animals
  • Anticonvulsants / pharmacology*
  • Anticonvulsants / toxicity
  • Behavior, Animal / drug effects*
  • Cyclohexanols / pharmacology*
  • Cyclohexanols / toxicity
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Electroshock
  • Formaldehyde
  • Lethal Dose 50
  • Male
  • Mice
  • Monoterpenes / pharmacology*
  • Monoterpenes / toxicity
  • Motor Activity
  • Nociception / drug effects*
  • Nociceptive Pain / chemically induced
  • Nociceptive Pain / physiopathology
  • Nociceptive Pain / prevention & control*
  • Nociceptive Pain / psychology
  • Pentylenetetrazole
  • Reaction Time / drug effects
  • Rotarod Performance Test
  • Seizures / chemically induced
  • Seizures / prevention & control*
  • Time Factors
  • Trityl Compounds / pharmacology*
  • Trityl Compounds / toxicity

Substances

  • Acyclic Monoterpenes
  • Analgesics
  • Anticonvulsants
  • Cyclohexanols
  • Monoterpenes
  • Trityl Compounds
  • Formaldehyde
  • linalool oxide
  • Acetic Acid
  • Pentylenetetrazole