Role of GABA(B) receptors in the sedative/hypnotic effect of gamma-hydroxybutyric acid
by
Carai MA, Colombo G, Brunetti G, Melis S, Serra S,
Vacca G, Mastinu S, Pistuddi AM, Solinas C,
Cignarella G, Minardi G, Gessa GL.
"Bernard B. Brodie" Department of Neuroscience,
University of Cagliari,
S.S. 554 Km. 4.5, I-09042 (CA),
Monserrato, Italy
Eur J Pharmacol 2001 Oct 12;428(3):315-21

ABSTRACT

The present study was aimed at identifying the receptor systems involved in the mediation of the sedative/hypnotic effect of gamma-hydroxybutyric acid (GHB) in DBA mice. Administration of the putative antagonist of the GHB binding site, 6,7,8,9-tetrahydro-5-hydroxy-5H-benzocyclohept-6-ylideneacetic acid (NCS-382; 50-500 mg/kg, i.p.), significantly increased the duration of loss of righting reflex induced by GHB (1000 mg/kg, i.p.). In contrast, the GABA(B) receptor antagonists, (2S)(+)-5,5-dimethyl-2-morpholineacetic acid (SCH 50911; 25-100 mg/kg, i.p.) and (3-aminopropyl)(cyclohexylmethyl)phosphinic acid (CGP 46381; 12.5-150 mg/kg, i.p.), completely prevented the sedative/hypnotic effect of GHB. SCH 50911 (100 and 300 mg/kg, i.p.) was also capable to readily reverse the sedative/hypnotic effect of GHB (1000 mg/kg, i.p.) in mice that had lost the righting reflex. SCH 50911 (100 mg/kg, i.p.) also completely abolished the sedative/hypnotic effect of the GABA(B) receptor agonist, baclofen. These results indicate that the sedative/hypnotic effect of GHB is mediated by the stimulation of GABA(B) receptors and add further support to the hypothesis that the GABA(B) receptor constitutes a central site of action of GHB.

GHB
GABA
MDMA
Opioids
Reward
Ethanol
Dopamine
GHB: structure
GHB withdrawal
GHB and cocaine
Drugs and reward
GHB and the brain
GHB and alcoholism
GHB and narcolepsy
GHB and growth hormone
The pleasure and the pain
GHB, GABA(A) and GABA(B)

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