γ-Hydroxybutyrate (GHB) is a four-carbon chain monocarboxylic acid that is naturally present in the mammalian central nervous system (CNS). GET-73, a GHB analog, shows effect on hippocampal glutamate transmission. The microdialysis results indicated that local perfusion (60 min) with 10 μM – 1 μM GET73 increased extracellular glutamate levels in the CA1 region of the hippocampus of freely moving rats in a concentration dependent manner. In tissue slices from the rat hippocampus, treatment with 1 μM GET73 significantly increased K+-evoked, but not spontaneous, glutamate efflux. Moreover, 500 nM GET73 partially but significantly counteracted the increase in K+-evoked glutamate efflux induced by 100 μM CHPG, an mGluR5 agonist. These findings demonstrate that the GHB analog GET73 significantly affects glutamate transmission in the hippocampus[3]. Interestingly, the addiction of GET73 (1 and 10 µM) 1 h before and during chronic ethanol exposure prevented all the ethanol-induced effects (such as: a reduction of cell viability, an alteration of cytoskeleton, a decrease in extracellular glutamate levels and an increase of reactive oxygen species production)[4].
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