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-B1018AS
    Phenelzine-d5 sulfate
    		Inhibitor 99.97%
    Phenelzine-d5 sulfate is the deuterium labeled Phenelzine sulfate (HY-B1018A). Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer.
    Phenelzine-d<sub>5</sub> sulfate
  • HY-19271
    NS-2710
    		Agonist 99.21%
    NS-2710 is a high-efficacy GABAAα3 agonist with a Ki of 9.2 nM. NS-2710 can be used for anxiety research.
    NS-2710
  • HY-N9506
    Anisatin
    		Antagonist 99.0%
    Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM.
    Anisatin
  • HY-114871
    SL651498
    		Antagonist
    SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities.
    SL651498
  • HY-124467
    Difludiazepam
    		98.9%
    Difludiazepam (Ro 07-4065), a benzodiazepine, has binding affinity (0.613) to GABAA receptors.
    Difludiazepam
  • HY-W005749
    (R)-4-Amino-3-hydroxybutyric acid
    		Agonist
    (R)-4-Amino-3-hydroxybutyric acid ((R)-GABOB) is a 4-aminobutyric acids (GABAB) agonist. (R)-4-Amino-3-hydroxybutyric acid is promising for research of nervous disorders.
    (R)-4-Amino-3-hydroxybutyric acid
  • HY-106025
    Radequinil
    		Antagonist 99.25%
    Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.
    Radequinil
  • HY-103527
    RuBi-GABA
    RuBi-GABA is a new ruthenium-based caged GABA compound. RuBi-GABA photocleaves and releases GABA after being excited with visible wavelengths. RuBi-GABA produces gaba receptor-mediated currents.
    RuBi-GABA
  • HY-119404
    Diproqualone
    		Agonist 99.9%
    diproqualone is methaqualone analogous with sedative, anxiolytic, anti-inflammatory and analgesic properties.
    Diproqualone
  • HY-P5964A
    K1 peptide TFA
    		Ligand 98.22%
    K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP).
    K1 peptide TFA
  • HY-110234
    Topiramate D12
    		Activator 99.90%
    Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
    Topiramate D12
  • HY-100799
    ZAPA sulfate
    		Agonist 99.25%
    ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM.
    ZAPA sulfate
  • HY-108034
    GET73
    		98.69%
    GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.
    GET73
  • HY-A0198
    Adinazolam
    		Agonist ≥99.0%
    Adinazolam (U 41123) is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities.
    Adinazolam
  • HY-10061
    Lesogaberan
    		Agonist
    Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan 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 inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan
  • HY-133486
    GABAA receptor agent 1
    		98.93%
    GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity.
    GABAA receptor agent 1
  • HY-100664
    Zopiclone N-oxide
    		Agonist ≥98.0%
    Zopiclone N-oxide (RP 29753) is a less active metabolite of Zopiclone. Zopiclone N-oxide is also an impurity of Eszopiclone and is formed by the oxidation of Eszopiclone.
    Zopiclone N-oxide
  • HY-163855
    KGP-25
    KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for general anesthesia.
    KGP-25
  • HY-154436
    Anticonvulsant agent 2
    		Inhibitor
    Anticonvulsant agent 2 is a potent and orally active anticonvulsant agent. Anticonvulsant agent 2 shows antiepileptic activity.
    Anticonvulsant agent 2
  • HY-19872
    AZD-6280
    		Modulator 99.09%
    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
    AZD-6280
Cat. No. Product Name / Synonyms Application Reactivity