Baclofen analgesia: involvement of the GABAergic system

Pharmacol Res. 2002 Sep;46(3):281-6. doi: 10.1016/s1043-6618(02)00147-0.

Abstract

The effect of baclofen, a GABA(B) agonist, has been studied in the hot plate test in mice, to analyze the possible involvement of the GABAergic system in baclofen analgesia. Baclofen (1-3 mg kg(-1) intraperitoneal (i.p.)) was found to elicit a dose-dependent antinociceptive effect. The antinociceptive effect of baclofen cannot be due to motor incoordination or sedation as the doses of baclofen which produce analgesia did not induce these effects during the rota-rod test. The antinociceptive effect of baclofen was reversed by 2-hydroxysaclofen, a GABA(B) antagonist by both systemic (3 mg kg(-1)) and intra cisterna magna (intracisternal (i.c.)) (0.3 mg kg(-1)) administration. The antagonist dose administered via i.c. produced a complete blockade and was 10-fold lower than the dose employed in i.p. administration. The data suggest that the antinociceptive effect of baclofen is GABA(B) receptor-mediated and reveal a central location of the analgesic effect of baclofen.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / pharmacology*
  • Animals
  • Baclofen / analogs & derivatives*
  • Baclofen / pharmacology*
  • Dose-Response Relationship, Drug
  • GABA Agonists / pharmacology*
  • GABA Antagonists / pharmacology
  • Injections, Intraperitoneal
  • Male
  • Mice
  • Muscle Relaxation / drug effects
  • Receptors, GABA / drug effects

Substances

  • Analgesics
  • GABA Agonists
  • GABA Antagonists
  • Receptors, GABA
  • Baclofen
  • 2-hydroxysaclofen