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-Y0313S1
    p-Hydroxybenzaldehyde-13C
    		Antagonist
    p-Hydroxybenzaldehyde-13C is the 13C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde-<sup>13</sup>C
  • HY-U00199A
    (S)-Norzopiclone
    		Agonist
    (S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABAA receptor and inhibits nACh and NMDA receptors.
    (S)-Norzopiclone
  • HY-111136
    BL-1020 mesylate
    		Agonist
    BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate.
    BL-1020 mesylate
  • HY-161896
    Transcription factor-IN-1
    		Inhibitor
    Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED50 =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models.
    Transcription factor-IN-1
  • HY-14758
    Adipiplon
    		Agonist
    Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.
    Adipiplon
  • HY-130349
    Emamectin B1a
    		Activator
    Emamectin B1a (L-656,748) is a semisynthetic derivative of avermectin B1a that binds to GABA receptors (Ki=17.6 nM in rat brain membranes) and enhances GABA responses. Emamectin B1a acitivates GABAA receptors α1β1γ2, α1β2γ2, and α1β3γ2 with IC50s of 57, 210, and 49.8 nM, respectively. Emamectin B1a also binds to glycine receptors, inhibiting glycine receptors with an IC50=218 nM in rat spinal cord. Emamectin B1a (1.067 ng/mL) caused 90% mortality of S. exigua larvae in foliar spray bioassays and topical application, making it more toxic than avermectin B1.
    Emamectin B1a
  • 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-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-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 99.95%
    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-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[1][2][3][4][5].
    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
Cat. No. Product Name / Synonyms Application Reactivity