GHB receptor

GHB receptor

G protein-coupled receptor 172A
Identifiers
Symbol GPR172A
Entrez HUGO OMIM RefSeq UniProt Locus q24.3

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

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 administration of mixed GHBR/GABAB 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]

Selective Ligands

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

Agonists

Antagonists

References