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-139584
    Temgicoluril
    		Inhibitor 98.03%
    Temgicoluril (Tetramethylglycoluril) is an orally active antianxiety and antidepressant. Temgicoluril acts on GABA receptors to enhance GABA neurotransmission.
    Temgicoluril
  • HY-103668A
    SSD114 hydrochloride
    		Agonist 99.13%
    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
    SSD114 hydrochloride
  • HY-P11208C
    mNLS-CPP-WSTF TFA
    		Inhibitor
    mNLS-CPP-WSTF TFA is the trifluoroacetate salt of mNLS-CPP-WSTF (HY-P11208). mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA.
    mNLS-CPP-WSTF TFA
  • HY-101639A
    CP-409092 hydrochloride
    		Agonist 99.79%
    CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity.
    CP-409092 hydrochloride
  • HY-137204
    COR659
    		Activator 99.94%
    COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats.
    COR659
  • 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 98.2%
    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-P5964A
    K1 peptide TFA
    		Ligand 98.59%
    K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP).
    K1 peptide TFA
  • HY-101060
    FGIN-1-43
    		Activator 98.96%
    FGIN-1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN-1-43
  • HY-101060
    FGIN-1-43
    		Inhibitor 98.96%
    FGIN-1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN-1-43
  • HY-141672S1
    17β-Estradiol sulfate-d4 sodium
    		99.57%
    17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.
    17β-Estradiol sulfate-d<sub>4</sub> sodium
  • HY-N2368B
    Arecaidine hydrobromide
    		Inhibitor 98.0%
    Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine hydrobromide
  • HY-19872
    AZD6280
    		Modulator 98.49%
    AZD6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
    AZD6280
  • HY-B1095
    Chlormadinone acetate
    		Ligand 98.0%
    Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders.
    Chlormadinone acetate
  • HY-P11208B
    mNLS-CPP-scramble TFA
    		Control 98.44%
    mNLS-CPP-scramble (TFA) is the trifluoroacetate salt of mNLS-CPP-scramble (HY-P11208A). mNLS-CPP-scramble is a negative control peptide of mNLS-CPP-WSTF. mNLS-CPP-scramble is promising for research of chronic inflammatory diseases (e.g., MASH, osteoarthritis).
    mNLS-CPP-scramble TFA
  • HY-124463
    Epiallopregnanolone
    		Antagonist
    Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer.
    Epiallopregnanolone
  • HY-106316
    CGS 20625
    		Agonist 99.80%
    CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 enhances GABA in Xenopus laevis oocytes . CGS 20625 can be used for the research of pentylenetetrazol-induced seizures and anxiety.
    CGS 20625
  • HY-131885
    RuBi-Glutamate hexafluorophosphate sodium
    		Inhibitor
    RuBi-Glutamate hexafluorophosphate sodium is a neuronal activator. RuBi-Glutamate hexafluorophosphate sodium photocleaves to release glutamate upon one- or two-photon excitation, activating glutamate receptors in cortical pyramidal neurons. RuBi-Glutamate hexafluorophosphate sodium reduces peak amplitude of evoked GABAergic inhibitory postsynaptic currents in its caged form. RuBi-Glutamate hexafluorophosphate sodium can be used for the research of Huntington's disease.
    RuBi-Glutamate hexafluorophosphate sodium
  • HY-121116
    CGS 8216
    		99.85%
    CGS 8216 is a non-benzodiazepine brain benzodiazepine receptor ligand that binds to rat forebrain membranes with high affinity and specificity. CGS 8216 also inhibits 3H-flunitrazepam (3H-FLU) binding to rat synaptosomal membranes and blocks 3H-FLU labeling of brain benzodiazepine receptors in vivo with potency equivalent to Diazepam.
    CGS 8216
  • HY-138014
    Cinazepam
    		Agonist 99.1%
    Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.
    Cinazepam
Cat. No. Product Name / Synonyms Application Reactivity