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Vol. 281, Issue 2, 753-760, 1997
-Hydroxybutyrate Conversion into GABA Induces Displacement of
GABAB Binding that is Blocked by Valproate and
Ethosuximide1
L.N.M.I.C, UPR 416 CNRS, Centre de Neurochimie, Strasbourg Cedex,
France
-Hydroxybutyrate (GHB) has been reported to be a ligand for
GABAB receptor(s), although with low or very low affinity
(IC50 = 150-796 µM). In addition, several reports argue
for a role of GHB via GABAB receptors in both
in vivo and in vitro electrophysiological experiments. In the present study, we demonstrate that the inhibition of GHB's conversion into GABA by rat brain membranes blocks the ability of GHB to interfere with GABAB binding. In
particular, the inhibition of GHB dehydrogenase by valproate or
ethosuximide and the blockade of GABA-T by aminooxyacetic acid induce
the disappearance of the GABA-like effect of GHB at GABAB,
but also at GABAA, receptors. This finding could explain
the misinterpretation of in vi
ro or in
vivo experiments where GHB possesses a GABA-like effect. But in
addition, it is postulated that the normal metabolism of GHB in brain
induces GABAB mechanisms that could be blocked by the
administration of valproate or ethosuximide.
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