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G protein-coupled receptor 172A
Identifiers
Symbol GPR172A
Entrez 79581
HUGO 30224
OMIM 607882
RefSeq NM_024531
UniProt Q9HAB3
Other data
Locus Chr. 8 q24.3

Gamma-hydroxybutyrate receptor or GHB receptor (GHBR), originally identified as GPR172A, is a G protein-coupled receptor that binds gamma-Hydroxybutyric acid (GHB).

Contents

History

The existence of a specific GHB receptor was predicted by observing the action of GHB and related compounds that primarily act on GABAB receptors, but also exhibit a range of effects which were found not to be produced by GABAB activity, and so were suspected of being produced by a novel and at the time unidentified receptor target. Following the discovery of the "orphan" G-protein coupled receptor GPR172A, it was subsequently found to be the GHB receptor whose existence had been previously predicted.[1] The rat GHB receptor was first cloned and characterised in 2003[2] followed by the human receptor in 2007.[3]

Function

The function of the GHB receptor appears to be quite different from that of the GABAB receptor. It shares no sequence homology with GABAB, and selective agonists for the GHB receptor which are not agonists at GABAB, or administration of mixed GHBR/GABAB agonists along with a selective GABAB antagonist, do not produce a sedative effect, instead causing a stimulant effect followed by convulsions at higher doses, thought to be mediated through increased Na+/K+ current and increased release of dopamine and glutamate.[4][5][6][7][8][9]

Selective Ligands

  • (R)-4-[4′-(2-iodobenzyloxy)phenyl]-GHB[10]
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Agonists

Antagonists

References

  1. ^ Snead OC (November 2000). "Evidence for a G protein-coupled gamma-hydroxybutyric acid receptor". J. Neurochem. 75 (5): 1986–96. doi:10.1046/j.1471-4159.2000.0751986.x. PMID 11032888.  
  2. ^ Andriamampandry C, Taleb O, Viry S, et al. (September 2003). "Cloning and characterization of a rat brain receptor that binds the endogenous neuromodulator gamma-hydroxybutyrate (GHB)". FASEB J. 17 (12): 1691–3. doi:10.1096/fj.02-0846fje. PMID 12958178.  
  3. ^ Andriamampandry C, Taleb O, Kemmel V, Humbert JP, Aunis D, Maitre M (March 2007). "Cloning and functional characterization of a gamma-hydroxybutyrate receptor identified in the human brain". FASEB J. 21 (3): 885–95. doi:10.1096/fj.06-6509com. PMID 17197387.  
  4. ^ Cash, C (1999). "γ-hydroxybutyrate receptor function studied by the modulation of nitric oxide synthase activity in rat frontal cortex punches". Biochemical Pharmacology 58 (11): 1815. doi:10.1016/S0006-2952(99)00265-8. PMID 10571257.  
  5. ^ Maitre M, Humbert JP, Kemmel V, Aunis D, Andriamampandry C (March 2005). "[A mechanism for gamma-hydroxybutyrate (GHB) as a drug and a substance of abuse [A mechanism for gamma-hydroxybutyrate (GHB) as a drug and a substance of abuse]"] (in French). Med Sci (Paris) 21 (3): 284–9. PMID 15745703. http://www.edk.fr/reserve/revues/ms_papier/e-docs/00/00/06/F7/document_article.md.  
  6. ^ Castelli MP, Ferraro L, Mocci I, et al. (November 2003). "Selective gamma-hydroxybutyric acid receptor ligands increase extracellular glutamate in the hippocampus, but fail to activate G protein and to produce the sedative/hypnotic effect of gamma-hydroxybutyric acid". J. Neurochem. 87 (3): 722–32. doi:10.1046/j.1471-4159.2003.02037.x. PMID 14535954.  
  7. ^ Castelli MP (November 2008). "Multi-faceted aspects of gamma-hydroxybutyric Acid: a neurotransmitter, therapeutic agent and drug of abuse". Mini Rev Med Chem 8 (12): 1188–202. doi:10.2174/138955708786141025. PMID 18855733.  
  8. ^ Crunelli V, Emri Z, Leresche N (February 2006). "Unravelling the brain targets of gamma-hydroxybutyric acid". Curr Opin Pharmacol 6 (1): 44–52. doi:10.1016/j.coph.2005.10.001. PMID 16368267.  
  9. ^ Carter LP, Koek W, France CP (October 2008). "Behavioral analyses of GHB: Receptor mechanisms". Pharmacol. Ther. 121 (1): 100–14. doi:10.1016/j.pharmthera.2008.10.003. PMID 19010351.  
  10. ^ Høg S, Wellendorph P, Nielsen B, et al. (2008). "Novel High-Affinity and Selective Biaromatic 4-Substituted gamma-Hydroxybutyric Acid (GHB) Analogues as GHB Ligands: Design, Synthesis, and Binding Studies". J. Med. Chem. 51 (24): 8088–95. doi:10.1021/jm801112u. PMID 19053823.  
  11. ^ Ticku MK, Mehta AK (October 2008). "Characterization and pharmacology of the GHB receptor". Annals of the New York Academy of Sciences 1139: 374–85. doi:10.1196/annals.1432.048. PMID 18991884.  

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