2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

GABA Receptor

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GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0067S
    γ-Aminobutyric acid-d6
    		Agonist 99.90%
    γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
    γ-Aminobutyric acid-d<sub>6</sub>
  • HY-B1122
    L-Cycloserine
    		Inhibitor 99.44%
    L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacterium tuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains.
    L-Cycloserine
  • HY-100813
    Saclofen
    		Antagonist 99.87%
    Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats.
    Saclofen
  • HY-10232
    THIP
    		Antagonist 99.93%
    THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
    THIP
  • HY-113320
    Etiocholanolone
    		Modulator 99.31%
    Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form.
    Etiocholanolone
  • HY-N0659
    Jujuboside A
    		Agonist 99.88%
    Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, a Chinese herbal medicine used to treat insomnia and anxiety.
    Jujuboside A
  • HY-17354
    (R)-Baclofen
    		Agonist 98.87%
    (R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist.
    (R)-Baclofen
  • HY-103504
    (S)-SNAP5114
    		Inhibitor 98.16%
    (S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant agent.
    (S)-SNAP5114
  • HY-N0042
    Ginsenoside Rc
    		Agonist ≥98.0%
    Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
    Ginsenoside Rc
  • HY-B0799
    Dihydroergotoxine mesylate
    		Modulator 99.88%
    Dihydroergotoxine mesylate is a series of alkaloid salt mixtures with high binding activity to GABAA receptors.
    Dihydroergotoxine mesylate
  • HY-129105
    Clomethiazole
    		Agonist 99.75%
    Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
    Clomethiazole
  • HY-N2079
    (-)-Securinine
    		Antagonist 99.93%
    (-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
    (-)-Securinine
  • HY-B1240
    Droperidol
    		Inhibitor 99.90%
    Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC50 values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties.
    Droperidol
  • HY-108689
    Broflanilide
    		Antagonist 99.36%
    Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
    Broflanilide
  • HY-16974
    Afoxolaner
    		Inhibitor 99.95%
    Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
    Afoxolaner
  • HY-103530
    CGP35348
    		Antagonist ≥98.0%
    CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.
    CGP35348
  • HY-B1671
    (+)-Kavain
    		99.98%
    (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
    (+)-Kavain
  • HY-116564
    Lotilaner
    		Antagonist 99.84%
    Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor.
    Lotilaner
  • HY-Y0313
    p-Hydroxybenzaldehyde
    		Antagonist 99.98%
    p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde
  • HY-100810
    Isoguvacine hydrochloride
    		Agonist 99.81%
    Isoguvacine hydrochloride is a GABA receptor agonist.
    Isoguvacine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity