GHB receptor
SLC52A2 | |||
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Identifiers | |||
Gene ontology | |||
Molecular function | |||
Cellular component | |||
Biological process | |||
Sources:Amigo / QuickGO |
Ensembl |
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UniProt | |||||||||
RefSeq (mRNA) |
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RefSeq (protein) |
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Location (UCSC) | Chr 8: 144.33 – 144.36 Mb | n/a | |||||||
PubMed search | [2] | [3] |
View/Edit Human | View/Edit Mouse |
The γ-hydroxybutyrate (GHB) receptor (GHBR), originally identified as GPR172A, is an excitatory
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.[4] The rat GHB receptor was first cloned and characterised in 2003,[5] followed by the human receptor in 2007.[6]
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).
Function
The function of the GHB receptor appears to be quite different from that of the GABAB receptor. It shares no
Ligands
Agonists
- 3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA)
- 4-(p-Chlorobenzyl)-GHB
- Aceburic acid
- γ-Hydroxybutyric acid (GHB)
- γ-Hydroxyvaleric acid (GHV; 4-methyl-GHB)
- NCS-356 (4-(4-chlorophenyl)-4-hydroxy-but-2-enoic acid, CAS# 430440-66-7)
- NCS-435 (4-(p-methoxybenzyl)-GHB)
- trans-Hydroxycrotonic acid (T-HCA)
- UMB66
- UMB68
- UMB72
- UMB86[16]
Antagonists
Prodrugs
- 1,4-Butanediol - metabolised into GHB by ADH and ALDH[18]
- γ-Valerolactone (GVL) – metabolised to GHV[22]
Unknown/unclear
- Amisulpride
- Levosulpiride
- Prochlorperazine
- (R)-4-[4′-(2-Iodobenzyloxy)phenyl]-GHB[23]
- Sulpiride
- Sultopride
References
- ^ a b c ENSG00000285112 GRCh38: Ensembl release 89: ENSG00000185803, ENSG00000285112 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- S2CID 84200461.
- S2CID 489179.
- ^ S2CID 6069832.
- S2CID 7116392.
- PMID 12740431.
- PMID 20463145.
- PMID 10571257.
- PMID 15745703.
- S2CID 82175813.
- PMID 18855733.
- PMID 16368267.
- PMID 19010351.
- S2CID 37091049.
- PMID 22753476.
- S2CID 54415695.
- PMID 10869868.
- ISBN 978-0-87893-534-5.
- ISBN 978-0-471-73954-8.
- PMID 23486087.
- PMID 19053823.