A comparison of the anti-nociceptive effects of voltage-activated Na+ channel blockers in the formalin test

Eur J Pharmacol. 2002 Jun 12;445(3):231-8. doi: 10.1016/s0014-2999(02)01765-x.

Abstract

We have used the rat formalin test to compare the anti-nociceptive properties of several voltage-activated Na(+) channel blockers. The antiarrhthymic mexiletine (37.5 and 50 mg/kg, i.p.) attenuated flinching behaviour in both first and second phases of the test compared with vehicle (P<0.05). The anti-convulsants lamotrigine (15 and 30 mg/kg, i.p.) and carbamazepine (20 mg/kg, i.p.) also inhibited second phase flinching behaviour compared with vehicle (P<0.05), although phenytoin (up to 40 mg/kg, i.p.) was without effect. Riluzole (5 mg/kg, i.p.), in contrast to lubeluzole (up to 10 mg/kg, i.p.) also inhibited second phase flinching behaviour compared with vehicle (P<0.05). When tested against an acute thermal nociceptive stimulus mexiletine, lubeluzole and riluzole exhibited anti-nociceptive effects. The anti-nociceptive doses used in the formalin test produced no motor impairment in the rotarod test. Thus, voltage-activated Na(+) channel blockers can attenuate nociceptive behaviour in the formalin test, and a specific mechanism of action on Na(+) channel function may be required for this to occur.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Male
  • Pain Measurement / drug effects*
  • Pain Measurement / methods
  • Rats
  • Rats, Sprague-Dawley
  • Sodium Channel Blockers / pharmacology*
  • Sodium Channels / physiology*

Substances

  • Analgesics
  • Sodium Channel Blockers
  • Sodium Channels