GHB receptor
| 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 |
The γ-hydroxybutyrate (GHB) receptor (GHBR), originally identified as GPR172A, is a G protein-coupled receptor (GPCR) that binds the neurotransmitter and psychoactive drug γ-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 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.[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 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.[4][5][6][7][8][9]
Ligands
Agonists
- 1,4-Butanediol
- 3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA)
- 4-(p-Chlorobenzyl)-GHB
- γ-Butyrolactone (GBL)
- γ-Hydroxybutyric acid (GHB)
- γ-Hydroxyvaleric acid (GHV; 4-methyl-GHB)
- γ-Valerolactone (GVL)
- trans-Hydroxycrotonic acid (T-HCA)
- Aceburic acid
- NCS-356 (4-(4-chlorophenyl)-4-hydroxy-but-2-enoic acid, CAS# 430440-66-7)
- NCS-435 (4-(p-methoxybenzyl)-GHB)
- UMB66
- UMB68
- UMB72
- UMB86[10]
Antagonists
Unknown/unclear
- (R)-4-[4′-(2-Iodobenzyloxy)phenyl]-GHB]][12]
- Amisulpride
- Levosulpiride
- Prochlorperazine
- Sulpiride
- Sultopride
References
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