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-12783A
    SCH 50911
    		Antagonist ≥98.0%
    SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
    SCH 50911
  • HY-B0340
    Nefiracetam
    		Activator 99.91%
    Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.
    Nefiracetam
  • HY-Y1683
    DL-Menthol
    		Activator ≥98.0%
    DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production.
    DL-Menthol
  • HY-100936
    Etazolate hydrochloride
    		Modulator 98.00%
    Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
    Etazolate hydrochloride
  • HY-N6648
    Cirsimaritin
    		99.23%
    Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin
  • HY-103505
    CL 218872
    		Agonist 98.01%
    CL 218872 is a selective and orally active benzodiazepine of α1 subunit-containing GABAAreceptor with a Ki of 130 nM. CL 218872 exerts anxiolytic and anticonvulsant in vivo.
    CL 218872
  • HY-131693A
    γ-Acetylenic GABA hydrochloride
    		Inhibitor 99.64%
    γ-Acetylenic GABA (GAG) hydrochloride is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA hydrochloride can increase the concentration of GABA in rat brain. γ-Acetylenic GABA (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    γ-Acetylenic GABA hydrochloride
  • HY-N0301
    Thiocolchicoside
    		Antagonist 99.54%
    Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
    Thiocolchicoside
  • HY-139427
    3-Methylglutaconic acid
    		99.60%
    3-Methylglutaconic acid is the major metabolites accumulating in 3-Methylglutaconic aciduria (MGTA). 3-Methylglutaconic acid can induce lipid oxidative damage and protein oxidative. 3-Methylglutaconic acid decreases the non-enzymatic antioxidant defenses in cerebral cortex supernatants to elicit oxidative stress in the cerebral cortex. 3-Methylglutaconic acid can be used for brain damage disease research.
    3-Methylglutaconic acid
  • HY-119687
    Bifenazate
    		Agonist 99.89%
    Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor. Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III.
    Bifenazate
  • HY-116622
    α5IA
    		Agonist
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential.
    α5IA
  • HY-19371
    Lorediplon
    		Modulator 99.88%
    Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
    Lorediplon
  • HY-N2080
    Songorine
    		Antagonist 99.69%
    Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
    Songorine
  • HY-103506
    NNC-711
    		Inhibitor 99.76%
    NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC50 values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity.
    NNC-711
  • HY-107489
    RO 4938581
    		Antagonist 99.30%
    RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
    RO 4938581
  • HY-10061B
    Lesogaberan hydrochloride
    		Agonist ≥98.0%
    Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan hydrochloride
  • HY-13694S1
    Methionine-d4
    		Activator ≥98.0%
    Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine-d<sub>4</sub>
  • HY-100369A
    DMCM hydrochloride
    		Inhibitor 99.07%
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.
    DMCM hydrochloride
  • HY-N6628
    6,2'-Dihydroxyflavone
    		Antagonist 99.54%
    6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
    6,2'-Dihydroxyflavone
  • HY-103520
    DS2
    		Activator 99.94%
    DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research.
    DS2
Cat. No. Product Name / Synonyms Application Reactivity