GHB receptor

Quality 0.50 · 2 views · Updated 2 months ago

GHB receptor coding gene in the species Homo sapiens

title: "GHB receptor" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["g-protein-coupled-receptors", "gamma-hydroxybutyric-acid"] description: "GHB receptor coding gene in the species Homo sapiens" topic_path: "general/g-protein-coupled-receptors" source: "https://en.wikipedia.org/wiki/GHB_receptor" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

::summary GHB receptor coding gene in the species Homo sapiens ::

The γ-hydroxybutyrate (GHB) receptor (GHBR), originally identified as GPR172A, is an excitatory G protein-coupled receptor (GPCR) that binds the neurotransmitter and psychoactive drug γ-hydroxybutyric acid (GHB). As solute carrier family 52 member 2 (SLC52A2), it is also a transporter for riboflavin.

History

The existence of a specific GHB receptor was predicted by observing the action of GHB and related compounds that primarily act on the GABAB receptor, 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. The rat GHB receptor was first cloned and characterised in 2003, followed by the human receptor in 2007.

Due to its many functions, this gene has a history of multiple discoveries. In 2002, data mining in the human genome found an incorrectly spliced form of this protein with eight transmembrane helices, and due to the presence of a G-protein binding site, it was correctly assumed to be a GPCR (as GCPR41). In 2003, it was first identified in its 11-transmembrane-helix full length, as a receptor for porcine endogenous retrovirus. The same protein was later identified as the GHB receptor in 2007. In 2009, it was identified as a riboflavin transporter, and sorted into SLC family 52 due to sequence similarity. The authors of the 2009 study were not aware of the 2007 study showing that it actually does function as a GPCR.

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 administration of mixed GHB/GABAB receptor agonists, along with a selective GABAB antagonist or selective agonists for the GHB receptor which are not agonists at GABAB, 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.

Ligands

Agonists

Antagonists

Prodrugs

Unknown/unclear

References

References

  1. (November 2000). "Evidence for a G protein-coupled gamma-hydroxybutyric acid receptor". Journal of Neurochemistry.
  2. (September 2003). "Cloning and characterization of a rat brain receptor that binds the endogenous neuromodulator gamma-hydroxybutyrate (GHB)". FASEB Journal.
  3. (March 2007). "Cloning and functional characterization of a gamma-hydroxybutyrate receptor identified in the human brain". FASEB Journal.
  4. (June 2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters.
  5. (May 2003). "Identification of receptors for pig endogenous retrovirus". Proceedings of the National Academy of Sciences of the United States of America.
  6. (July 2010). "Identification and comparative functional characterization of a new human riboflavin transporter hRFT3 expressed in the brain". The Journal of Nutrition.
  7. (December 1999). "Gamma-hydroxybutyrate receptor function studied by the modulation of nitric oxide synthase activity in rat frontal cortex punches". Biochemical Pharmacology.
  8. (March 2005). "[A mechanism for gamma-hydroxybutyrate (GHB) as a drug and a substance of abuse]". Médecine/Sciences.
  9. (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". Journal of Neurochemistry.
  10. (October 2008). "Multi-faceted aspects of gamma-hydroxybutyric acid: a neurotransmitter, therapeutic agent and drug of abuse". Mini Reviews in Medicinal Chemistry.
  11. (February 2006). "Unravelling the brain targets of gamma-hydroxybutyric acid". Current Opinion in Pharmacology.
  12. (January 2009). "Behavioral analyses of GHB: receptor mechanisms". Pharmacology & Therapeutics.
  13. (October 2008). "Characterization and pharmacology of the GHB receptor". Annals of the New York Academy of Sciences.
  14. (August 2012). "α4βδ GABA(A) receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)". Proceedings of the National Academy of Sciences of the United States of America.
  15. (January 1984). "1,4 Butanediol, gamma-hydroxybutyric acid and ethanol: relationships and interactions". Neuropharmacology.
  16. (April 2000). "Abuse and therapeutic potential of gamma-hydroxybutyric acid". Alcohol.
  17. (2005). "Psychopharmacology: Drugs, the Brain and Behavior". Sinauer.
  18. (2011-11-29). "Forensic Chemistry Handbook". John Wiley & Sons.
  19. (May 2013). "Uptake of gamma-valerolactone--detection of gamma-hydroxyvaleric acid in human urine samples". Journal of Analytical Toxicology.
  20. (December 2008). "Novel high-affinity and selective biaromatic 4-substituted gamma-hydroxybutyric acid (GHB) analogues as GHB ligands: design, synthesis, and binding studies". Journal of Medicinal Chemistry.

::callout[type=info title="Wikipedia Source"] This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page. ::

g-protein-coupled-receptorsgamma-hydroxybutyric-acid