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-103524
    Valerenic acid
    		Activator ≥99.0%
    Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.
    Valerenic acid
  • HY-Y1176
    Isonipecotic acid
    		Agonist 99.93%
    Isonipecotic acid is a GABAA receptor partial agonist.
    Isonipecotic acid
  • HY-100369A
    DMCM hydrochloride
    		Inhibitor 99.07%
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.
    DMCM hydrochloride
  • HY-116622
    α5IA
    		Agonist
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential.
    α5IA
  • HY-N6628
    6,2'-Dihydroxyflavone
    		Antagonist 99.54%
    6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
    6,2'-Dihydroxyflavone
  • HY-103520
    DS2
    		Activator 99.94%
    DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research.
    DS2
  • HY-19945
    DAA-1106
    		Agonist 99.93%
    DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
    DAA-1106
  • HY-103475
    GS39783
    		Agonist 99.72%
    GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction.
    GS39783
  • HY-N2080
    Songorine
    		Antagonist 99.69%
    Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
    Songorine
  • HY-W012738
    DL-Pyroglutamic acid
    		Inhibitor ≥98.0%
    DL-Pyroglutamic acid (CAE) as an inactivator of hepatitis B surface, inactivates vaccinia virus, herpes simplex virus, and influenza virus except poliovirus. DL-Pyroglutamic acid is also a possible inhibitor of GABA transaminase, increases GABA amount with antiepileptic action.
    DL-Pyroglutamic acid
  • HY-100798
    Phaclofen
    		Antagonist 99.98%
    Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.
    Phaclofen
  • HY-129636
    CLH304a
    		Antagonist
    CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor.
    CLH304a
  • HY-100783
    (-)-Bicuculline methobromide
    		Antagonist 99.94%
    (-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca2+-activated K+ channels in various types of neurons.
    (-)-Bicuculline methobromide
  • HY-N0067S3
    γ-Aminobutyric acid-13C4
    		Agonist ≥99.0%
    γ-Aminobutyric acid-13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
    γ-Aminobutyric acid-<sup>13</sup>C<sub>4</sub>
  • HY-107198
    (2S)-6-Prenylnaringenin
    		Agonist 99.84%
    (2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface.
    (2S)-6-Prenylnaringenin
  • HY-A0173
    Progabide
    		Agonist 99.42%
    Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.
    Progabide
  • HY-13694S
    Methionine-d3
    		Activator 99.22%
    Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine-d<sub>3</sub>
  • HY-103528
    SCS
    		Inhibitor 99.64%
    SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions.
    SCS
  • HY-105791
    Sulazepam
    		99.56%
    Sulazepam, a benzodiazepine, is a selective ovarian cancer G protein-coupled receptor (OGR1) agonist. Sulazepam has anticonvulsive action and has the potential for airway hyperresponsiveness (AHR) research.
    Sulazepam
  • HY-103511
    TCS1105
    		99.66%
    TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion.
    TCS1105
Cat. No. Product Name / Synonyms Application Reactivity