Gamma-hydroxybutyrate is a weak agonist
at recombinant GABA(B) receptors
by
Lingenhoehl K, Brom R, Heid J, Beck P,
Froestl W, Kaupmann K, Bettler B, Mosbacher J
Nervous System Research,
Novartis Pharma AG,
Basel, Switzerland.
Neuropharmacology 1999 Nov; 38(11):1667-73

ABSTRACT

Gamma-hydroxybutyrate (GHB) is a neuromodulator with high affinity binding sites in the mammalian brain. However, the receptor for GHB has not yet been identified. There are indications that GHB and gamma-aminobutyric acid (GABA) mediate their effects via the same receptor. We tested this hypothesis using GABA(B)R1/R2 receptors co-expressed with Kir3 channels in Xenopus oocytes. GHB activated these receptors with an EC50 of approximately 5 mM and a maximal stimulation of 69% when compared to the GABA(B) receptor agonist L-baclofen. GHB and L-baclofen did not amplify each others effect nor did they stimulate the GABA(B) receptor in a linearly additive manner. CGP54626A, 2-OH saclofen and CGP35348, three competitive GABA(B) receptor antagonists, inhibited the GHB induced response completely. A concentration of 30 mM GHB displaced [125I]CGP64213 binding at GABA(B)R1 expressed in COS cells by 21%. These results indicate that GHB is a weak partial agonist at the GABA binding site of GABA(B)R1/R2.

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GHB, GABA(A) and GABA(B)
GABA, pain and the cerebral cortex
GABA(B) receptor function and antidepressant activity

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