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-12461
    WS6
    		Activator 99.94%
    WS6 is an IkB kinase and EBP1 inhibitor, with IC50 values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats[1][2][4].
    WS6
  • HY-B0339
    Primidone
    		Antagonist 99.96%
    Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.
    Primidone
  • 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-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-17354
    (R)-Baclofen
    		Agonist 99.50%
    (R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist.
    (R)-Baclofen
  • 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-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-B0171
    Antipyrine
    		Activator 99.98%
    Antipyrine (Phenazone) is an orally active antipyretic and analgesic. Antipyrine can be used as a probe agent for oxidative agent metabolism. Antipyrine also delays gastric emptying (GE) in rats.
    Antipyrine
  • HY-100810
    Isoguvacine hydrochloride
    		Agonist 99.81%
    Isoguvacine hydrochloride is a GABA receptor agonist.
    Isoguvacine hydrochloride
  • 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-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-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-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-B1494
    Picrotoxinin
    		Antagonist 99.82%
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
    Picrotoxinin
  • HY-129105
    Clomethiazole
    		Agonist 98.65%
    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-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-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-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-N0700
    alpha-Asarone
    		Activator 99.88%
    alpha-Asarone (α-Asarone) is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.
    alpha-Asarone
  • HY-103474
    Bicuculline methiodide
    		Inhibitor 99.24%
    Bicuculline methiodide is a potent GABA(A) receptors blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
    Bicuculline methiodide
Cat. No. Product Name / Synonyms Application Reactivity