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-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-W033027
    BGT1-IN-1
    		Inhibitor
    BGT1-IN-1 (compound 9) is a potent BGT1 inhibitor with IC50 value of 13.9, 58.3 µM for hBGT1, GAT3, respectively. BGT1-IN-1 shows no cytotoxic. BGT1-IN-1 shows neuroprotective activity.
    BGT1-IN-1
  • 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 is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
    Tiagabine hydrochloride (Standard)
  • 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-16974R
    Afoxolaner (Standard)
    		Inhibitor
    Afoxolaner (Standard) is the analytical standard of Afoxolaner. This product is intended for research and analytical applications. 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 (Standard)
  • HY-Y0313R
    p-Hydroxybenzaldehyde (Standard)
    		Antagonist
    p-Hydroxybenzaldehyde (Standard) is the analytical standard of p-Hydroxybenzaldehyde. This product is intended for research and analytical applications. 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 (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
    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-158252S
    Tiagabine-d5 hydrochloride
    		Inhibitor
    Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
    Tiagabine-d<sub>5</sub> hydrochloride
  • 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-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
  • HY-B1671R
    (+)-Kavain (Standard)
    (+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-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 (Standard)
  • HY-103535
    GBLD345
    		Agonist
    GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM).
    GBLD345
  • HY-B1715R
    Oxiracetam (Standard)
    		Agonist
    Oxiracetam (Standard) is the analytical standard of Oxiracetam. This product is intended for research and analytical applications. Oxiracetam (ISF2522) is an orally active and a BBB-penetrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases.
    Oxiracetam (Standard)
Cat. No. Product Name / Synonyms Application Reactivity