CGP 35348, a new GABAB antagonist, prevents antinociception and muscle-relaxant effect induced by baclofen

Br J Pharmacol. 1991 Jun;103(2):1303-8. doi: 10.1111/j.1476-5381.1991.tb09784.x.

Abstract

1. CGP 35348, a new GABAB antagonist, was examined on antinociception induced by (+/-)-baclofen by use of the hot plate and writhing tests in mice and the paw pressure test in rats. CGP 35348 was also studied in mice on (+/-)-baclofen-induced impairment of rota-rod performance. 2. CGP 35348, injected either i.p. (60-100 mg kg-1 in mouse) or intracerebroventricularly (i.c.v.) (0.5-2.5 micrograms per mouse; 25 micrograms per rat) prevented (+/-)-baclofen-induced antinociception. 3. CGP 35348 did not modify oxotremorine- and morphine-induced antinociception in mice and rats. 4. CGP 35348 (2.5 micrograms i.c.v. per mouse) also prevented (+/-)-baclofen-induced impairment of the rota-rod test. 5. Two other GABAB antagonists, phaclofen (50 micrograms i.c.v. per mouse) and 2-OH-saclofen (2.5 micrograms-10 micrograms i.c.v. per mouse) did not modify (+/-)-baclofen-induced antinociception. 7. These results suggest that, at present, CGP 35348 is the only compound able to antagonize (+/-)-baclofen-induced antinociception.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / antagonists & inhibitors*
  • Analgesics / pharmacology
  • Animals
  • Baclofen / analogs & derivatives
  • Baclofen / antagonists & inhibitors*
  • Baclofen / pharmacology
  • GABA Antagonists*
  • GABA-A Receptor Antagonists*
  • Injections, Intraventricular
  • Male
  • Mice
  • Morphine / pharmacology
  • Muscle Relaxation / drug effects
  • Muscles / drug effects*
  • Organophosphorus Compounds / pharmacology*
  • Oxotremorine / pharmacology
  • Postural Balance / drug effects
  • Rats
  • Rats, Inbred Strains
  • Reaction Time / drug effects

Substances

  • Analgesics
  • GABA Antagonists
  • GABA-A Receptor Antagonists
  • Organophosphorus Compounds
  • phaclofen
  • Oxotremorine
  • Morphine
  • CGP 35348
  • Baclofen
  • 2-hydroxysaclofen