GHB receptor

gamma-hydroxybutyrate receptorGHBGHB High
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).wikipedia
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Gamma-Hydroxybutyric acid

GHBγ-hydroxybutyric acidgamma-hydroxybutyrate
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).
It acts on the GHB receptor and is a weak agonist at the GABA B receptor.

HOCPCA

3-Hydroxycyclopent-1-enecarboxylic acid
3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA)
HOCPCA (3-hydroxycyclopent-1-enecarboxylic acid) is a compound with an affinity for the GHB receptor 39 times greater than that of GHB itself.

Psychoactive drug

psychoactivepsychotropicdrug
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).

T-HCA

T-HCA/GHCtrans''-Hydroxycrotonic acid
trans-Hydroxycrotonic acid (T-HCA)
trans-4-Hydroxycrotonic acid (T-HCA), also known as γ-hydroxycrotonic acid (GHC), is an agent used in scientific research to study the GHB receptor.

UMB66

3-chloropropanoic acid
UMB66
It is structurally related to GHB and binds to the GHB receptor, but has no affinity for GABA receptors.

NCS-382

4-Hydroxy-4-methylpentanoic acid

UMB68
UMB68
UMB68 has been shown to bind selectively to the GHB receptor ligand in binding assays, yet does not bind to GABAergic receptors.

Amisulpride

Amisulpride
Amisulpride and its relatives sulpiride, levosulpiride, and sultopride have been shown to bind to the high-affinity GHB receptor at concentrations that are therapeutically relevant (IC 50 = 50 nM for amisulpride).

Sulpiride

sandulpiride
Sulpiride
The benzamide neuroleptics (including sulpiride, amisulpride, and sultopride) have been shown to activate the endogenous gamma-hydroxybutyrate receptor in vivo at therapeutic concentrations.

Gabazine

Gabazine (SR-95531)
Gabazine has been found to bind to and antagonize α 4 βδ subunit-containing GABA A receptors, which may represent the GHB receptor.

Sultopride

Sultopride
It has also been shown to have clinically relevant affinity for the GHB receptor as well, a property it shares in common with amisulpride and sulpiride.

G protein-coupled receptor

G protein-coupled receptorsGPCRG protein-coupled
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).

Neurotransmitter

neurotransmittersexcitatory neurotransmitterneurotransmitter system
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).

GABAB receptor

GABA B receptorGABA B GABA B receptors
The existence of a specific GHB receptor was predicted by observing the action of GHB and related compounds that primarily act on the GABA B receptor, but also exhibit a range of effects which were found not to be produced by GABA B activity, and so were suspected of being produced by a novel and at the time unidentified receptor target.

Sequence homology

orthologparalogsparalog
It shares no sequence homology with GABA B, and administration of mixed GHB/GABA B receptor agonists along with a selective GABA B antagonist or selective agonists for the GHB receptor which are not agonists at GABA B, 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.

Convulsion

convulsionsconvulsiveconvulsing
It shares no sequence homology with GABA B, and administration of mixed GHB/GABA B receptor agonists along with a selective GABA B antagonist or selective agonists for the GHB receptor which are not agonists at GABA B, 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.

Dopamine

DAdopaminergic systemdopaminergic
It shares no sequence homology with GABA B, and administration of mixed GHB/GABA B receptor agonists along with a selective GABA B antagonist or selective agonists for the GHB receptor which are not agonists at GABA B, 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.

Glutamic acid

glutamateGluglutamate metabolism
It shares no sequence homology with GABA B, and administration of mixed GHB/GABA B receptor agonists along with a selective GABA B antagonist or selective agonists for the GHB receptor which are not agonists at GABA B, 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.

Gamma-Hydroxyvaleric acid

γ-Hydroxyvaleric acidgamma''-Hydroxyvaleric acid4-methyl-GHB
γ-Hydroxyvaleric acid (GHV; 4-methyl-GHB)

Gamma-Valerolactone

γ-Valerolactonegamma''-Valerolactonegamma-valerolactones
γ-Valerolactone (GVL)