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

Related Products

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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-114811
    Leptophos oxon
    		Inhibitor
    Leptophos oxon, a metabolite of leptophos, is a GABAA receptor chloride channel inhibitor with an IC50 values of 89.6 μM. Leptophos oxon inhibits GABA-induced chloride influx, binds to GABAA receptor-associated TBPS sites, and inhibits TBPS binding to voltage-dependent chloride channels. Leptophos oxon is a insecticide. Leptophos oxon can be used for the research of neurological disease.
    Leptophos oxon
  • HY-15399R
    Vigabatrin (Standard)
    		Inhibitor
    Vigabatrin (Standard) is the analytical standard of Vigabatrin. This product is intended for research and analytical applications. Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
    Vigabatrin (Standard)
  • HY-B1803
    Tracazolate
    		Activator
    Tracazolate (ICI 136753) is an orally active non-benzodiazepine anxiolytic. Tracazolate significantly enhances the binding of the radioligand 3H-flunitrazepam (3H-FLU) to brain tissue benzodiazepine receptors. Tracazolate enhances the binding of γ-aminobutyric acid (GABA) to its receptors. Tracazolate exhibits anticonvulsant activity. Tracazolate can be used in anxiety-related research.
    Tracazolate
  • HY-183357
    GABAAR/5-HT2AR modulator-1
    		Agonist
    GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABAAR agonist and 5-HT2AR antagonist with Kd values of 0.89 and 0.78 μM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-α, IL-6, IL-1β, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-κB pathway activation by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage.
    GABAAR/5-HT2AR modulator-1
  • HY-179519
    Umbelopsisin A
    		Agonist
    Umbelopsisin A is a GABAA and GABAB non-selective agonist. Umbelopsisin A activates the GABAergic pathway, including notch signaling and fatty acid metabolism. Umbelopsisin A shows dual neuroprotection against glutamate excitotoxicity in vitro (reducing ROS and cell death) and in vivo. Umbelopsisin A can be used for the study of glaucoma and broader neurodegenerative disease applications.
    Umbelopsisin A
  • HY-109572
    GABAA receptor modulator-1
    		Modulator
    GABAA receptor modulator-1 (9eey) is a GABAA receptor modulator that can be used in the study of central nervous system diseases.
    GABAA receptor modulator-1
  • HY-W103105R
    R 29676 (Standard)
    		Antagonist
    R 29676 is a neuroleptic agent and inhibits sodium-dependent GABA binding (GABA uptake).
    R 29676 (Standard)
  • HY-146282
    mGAT-IN-1
    		Inhibitor
    mGAT-IN-1 (compound 28) is a potent and non-selective GAT inhibitor. mGAT-IN-1 has a high inhibitory potency toward mGAT3, with an IC50 of 2.5 μM and pIC50 of 5.61.
    mGAT-IN-1
  • HY-B0696AR
    Tiagabine hydrochloride (Standard)
    		Inhibitor
    Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
    Tiagabine hydrochloride (Standard)
  • HY-N15436
    5-Deoxykievitone
    		Modulator
    5-Deoxykievitone, an isoflavanone found in Phaseolus species, is a GABA receptor modulator. 5-Deoxykievitone potentiates GABA-induced chloride current through α1β2γ2s GABAA receptors. 5-Deoxykievitone can be used for the research of epilepsy and anxiety.
    5-Deoxykievitone
  • HY-B0211AR
    Riluzole hydrochloride (Standard)
    		Inhibitor
    Riluzole hydrochloride (Standard) is the analytical standard of Riluzole hydrochloride. This product is intended for research and analytical applications. Riluzole hydrochloride is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
    Riluzole hydrochloride (Standard)
  • HY-103533R
    Gabazine (Standard)
    		Antagonist
    Gabazine (Standard) is the analytical standard of Gabazine. This product is intended for research and analytical applications. Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
    Gabazine (Standard)
  • HY-107994R
    Aminooxyacetic acid hemihydrochloride (Standard)
    		Inhibitor
    Aminooxyacetic acid (hemihydrochloride) (Standard) is the analytical standard of Aminooxyacetic acid (hemihydrochloride). This product is intended for research and analytical applications. Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
    Aminooxyacetic acid hemihydrochloride (Standard)
  • HY-169651
    GABA-IN-4
    GABA-IN-4 (Compound 17) is a N-(indol-3-ylglyoxylyl)benzylamine derivative. GABA-IN-4 exhibits high affinity for the benzodiazepine receptor (BzR) (binding site in GABAA receptor complex) with Ki value of 67 nM. Benzodiazepines are widely used as antianxiety, sedative-hypnotic and anticonvulsant agents.
    GABA-IN-4
  • HY-100140A
    Pipequaline hydrochloride
    		Agonist 99.69%
    Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline hydrochloride
  • HY-100936R
    Etazolate hydrochloride (Standard)
    		Modulator
    Etazolate (hydrochloride) (Standard) is the analytical standard of Etazolate (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-109009AR
    (S)-Padsevonil (Standard)
    		Modulator
    (S)-Padsevonil (Standard) is the analytical standard of (S)-Padsevonil (HY-109009A). This product is intended for research and analytical applications. (S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
    (S)-Padsevonil (Standard)
  • HY-B0211S1
    Riluzole-13C6
    		Inhibitor
    Riluzole-13C6 (PK 26124-13C6) is 13C labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
    Riluzole-<sup>13</sup>C<sub>6</sub>
  • HY-109009R
    Padsevonil (Standard)
    Padsevonil (Standard) is the analytical standard of Padsevonil (HY-109009). This product is intended for research and analytical applications. Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
    Padsevonil (Standard)
  • HY-125508
    CCD-3693
    		Agonist
    CCD-3693 is an orally active GABA receptor agonist. CCD-3693 has anxiolytic, anticonvulsant and sedative hypnotic activities and can be used in research related to neurological diseases.
    CCD-3693
Cat. No. Product Name / Synonyms Application Reactivity