γ-Hydroxybutyric acid (GHB) and γ-aminobutyric acidB receptor (GABABR) binding sites are distinctive from one another: molecular evidence
@article{Wu2004HydroxybutyricA,
title={$\gamma$-Hydroxybutyric acid (GHB) and $\gamma$-aminobutyric acidB receptor (GABABR) binding sites are distinctive from one another: molecular evidence},
author={Ying Wu and Saima Ali and Gholamreza Ahmadian and Chun Che Liu and Yu Tian Wang and Kenneth Michael Gibson and Andrew R. Calver and Joseph Francis and Menelas N. Pangalos and O. Carter Snead},
journal={Neuropharmacology},
year={2004},
volume={47},
pages={1146-1156}
}54 Citations
Novel Cyclic γ-Hydroxybutyrate (GHB) Analogs with High Affinity and Stereoselectivity of Binding to GHB Sites in Rat Brain
- Chemistry, BiologyJournal of Pharmacology and Experimental Therapeutics
- 2005
Three conformationally restricted GHB analogs are synthesized and assayed for binding against the GHB-specific ligand [3H]NCS-382 in rat brain homogenate and show excellent potential as lead structures and novel tools for studying specific GHB receptor-mediated pharmacology.
Novel Radioiodinated γ-Hydroxybutyric Acid Analogues for Radiolabeling and Photolinking of High-Affinity γ-Hydroxybutyric Acid Binding Sites
- Biology, ChemistryJournal of Pharmacology and Experimental Therapeutics
- 2010
A 125I-labeled photoaffinity derivative of the new GHB ligand is developed and is a useful tool for in vitro studies of the specific high-affinity GHB binding sites and can be used as a probe for isolation of the elusiveGHB binding protein.
γ-Hydroxybutyrate (GHB) induces GABAB receptor independent intracellular Ca2+ transients in astrocytes, but has no effect on GHB or GABAB receptors of medium spiny neurons in the nucleus accumbens
- BiologyNeuroscience
- 2009
Drosophila GABAB receptors are involved in behavioral effects of γ-hydroxybutyric acid (GHB)
- Biology
- 2005
Phenylacetic acids and the structurally related non‐steroidal anti‐inflammatory drug diclofenac bind to specific γ‐hydroxybutyric acid sites in rat brain
- Biology, ChemistryFundamental & clinical pharmacology
- 2009
Measuring the affinities of structurally related NSAIDs for the [3H]NCS‐382 site identified diclofenac, a clinically relevant NSAID of the phenylacetic acid (PAA) type, as a GHB ligand (Ki value of 5.1 μm), and other non‐NSAID PAAs also exhibited affinity similar to GHB.
GABAB Receptor-Positive Modulators: Brain Region-Dependent Effects
- Biology, ChemistryJournal of Pharmacology and Experimental Therapeutics
- 2012
The results show that GABAB receptor-positive modulators enhance [35S]GTPγS binding stimulated by GABAB receptors agonists in a brain region-dependent manner, possibly allowing for more selective therapeutic targeting of the GABAB system.
GHB receptor targets in the CNS: focus on high-affinity binding sites.
- Biology, ChemistryBiochemical pharmacology
- 2014
Succinic Semialdehyde Dehydrogenase Deficiency: GABAB receptor-mediated function
- BiologyBrain Research
- 2006
References
SHOWING 1-10 OF 41 REFERENCES
Stereoselectivity of NCS-382 binding to γ-hydroxybutyrate receptor in the rat brain
- Chemistry, Biology
- 2002
Specific γ‐hydroxybutyrate‐binding sites but loss of pharmacological effects of γ‐hydroxybutyrate in GABAB(1)‐deficient mice
- Biology, Chemistry
- 2003
It appears that all studied GHB effects are GABAB receptor dependent, and the GHB‐induced GTPγ[35S] responses are mediated by GABAB receptors.
Binding characteristics of the gamma-hydroxybutyric acid receptor antagonist [(3)H](2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid in the rat brain.
- Biology, ChemistryThe Journal of pharmacology and experimental therapeutics
- 2001
Radioligand binding studies with [(3)H](2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid ([(3)H]NCS-382), an antagonist of gamma-hydroxybutyric acid (GHB) receptor,…
The ontogeny of [3H]γ-hydroxybutyrate and [3H]GABA B binding sites: relation to the development of experimental absence seizures
- BiologyBrain Research
- 1994
gamma-Hydroxybutyrate conversion into GABA induces displacement of GABAB binding that is blocked by valproate and ethosuximide.
- BiologyThe Journal of pharmacology and experimental therapeutics
- 1997
It is demonstrated that the inhibition of GHB's conversion into GABA by rat brain membranes blocks the ability ofGHB to interfere with GABAB binding, which could explain the misinterpretation of in vitro or in vivo experiments where GHB possesses a GABA-like effect.
Quantitative autoradiographic analysis of the new radioligand [3H](2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid ([3H]NCS-382) at γ-hydroxybutyric acid (GHB) binding sites in rat brain
- Biology, ChemistryBrain Research
- 2003
Evidence for a G Protein‐Coupled γ‐Hydroxybutyric Acid Receptor
- Biology, Chemistry
- 2000
The hypothesis that GHB induces a Gprotein‐mediated decrease in adenylyl cyclase via a GHB‐specific G protein‐coupled presynaptic receptor that is different from the GABABR is supported.