gamma-Hydroxybutyric acid and baclofen decrease extracellular acetylcholine levels in the hippocampus via GABA(B) receptors

Eur J Pharmacol. 2001 Nov 2;430(2-3):261-3. doi: 10.1016/s0014-2999(01)01163-3.

Abstract

The effect of gamma-hydroxybutyric acid (GHB) and baclofen, a GABA(B) receptor agonist, on extracellular hippocampal acetylcholine levels was studied in freely moving rats by microdialysis. GHB (200 and 500 mg/kg, i.p.) reduced in a dose-dependent manner, extracellular hippocampal acetylcholine concentrations and this effect was prevented by the GABA(B) receptor antagonist (2S)(+)-5,5-Dimethyl-2-morpholineacetic acid (SCH 50911), at the dose of 20 mg/kg (i.p.), while the putative GHB receptor antagonist 6,7,8,9-Tetrahydro-5-hydroxy-5H-benzocyclohept-6-ylideneacetic acid (NCS 382) was ineffective. Similar to GHB, the GABA(B) agonist baclofen (10 and 20 mg/kg, i.p.) produced a dose-related reduction in extracellular acetylcholine concentrations which was prevented by SCH 50911. These findings indicate that GHB-induced reduction of hippocampal acetylcholine release is mediated by GABA(B) receptors and support a possible involvement of hippocampal GABA(B) receptors in the control of cognitive processes and in the claimed amnesic effect of GHB intoxication.

MeSH terms

  • Acetylcholine / metabolism*
  • Animals
  • Anticonvulsants / pharmacology
  • Baclofen / pharmacology*
  • Benzocycloheptenes / pharmacology
  • Dose-Response Relationship, Drug
  • Extracellular Space / drug effects
  • Extracellular Space / metabolism
  • GABA Agonists / pharmacology*
  • GABA Antagonists / pharmacology
  • Hippocampus / drug effects*
  • Hippocampus / metabolism
  • Hydroxybutyrates / pharmacology*
  • Male
  • Morpholines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, GABA-B / physiology*
  • Time Factors

Substances

  • (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid
  • Anticonvulsants
  • Benzocycloheptenes
  • GABA Agonists
  • GABA Antagonists
  • Hydroxybutyrates
  • Morpholines
  • Receptors, GABA-B
  • NCS 382
  • 4-hydroxybutyric acid
  • Baclofen
  • Acetylcholine