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-113346
    Tetrahydrodeoxycorticosterone
    		Agonist 99.45%
    Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.
    Tetrahydrodeoxycorticosterone
  • HY-W012738S
    DL-Pyroglutamic acid-d5
    		99.21%
    DL-Pyroglutamic acid-d5 is the deuterium labeled DL-Pyroglutamic acid.
    DL-Pyroglutamic acid-d<sub>5</sub>
  • HY-10061B
    Lesogaberan hydrochloride
    		Agonist 98.0%
    Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride 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 hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan hydrochloride
  • 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-114883A
    Homocarnosine TFA
    		99.83%
    Homocarnosine TFA is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine TFA is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects. Homocarnosine TFA has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.
    Homocarnosine TFA
  • HY-100370
    MRK-016
    		Antagonist 99.71%
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
    MRK-016
  • 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-16579
    Etifoxine hydrochloride
    		Activator 99.87%
    Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
    Etifoxine hydrochloride
  • HY-N7110
    6-Hydroxyflavone
    		99.92%
    6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role.
    6-Hydroxyflavone
  • HY-W041333
    Phenibut hydrochloride
    		Agonist 98.0%
    Phenibut (β-Phenyl-GABA) hydrochloride is an orally active GABA-B agonist. Phenibut hydrochloride acts as a GABA-mimetic, primarily at GABAB?receptors. Phenibut hydrochloride has anxiolytic and nootropic (cognition enhancing) effects.
    Phenibut hydrochloride
  • HY-100783
    (-)-Bicuculline methobromide
    		Antagonist 99.94%
    (-)-Bicuculline methobromide is a potent GABAA blocker. (-)-Bicuculline methobromide alters membrane properties and firing pattern. (-)-Bicuculline methobromide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. (-)-Bicuculline methobromide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
    (-)-Bicuculline methobromide
  • HY-103476
    Ro15-4513
    		Antagonist 99.17%
    Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect. Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Ro15-4513
  • HY-N6648
    Cirsimaritin
    		99.23%
    Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin
  • HY-A0173
    Progabide
    		Agonist 98.50%
    Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.
    Progabide
  • HY-103505
    CL 218872
    		Modulator 99.25%
    CL 218872 is an orally active and selective ligand for the benzodiazepine receptor subtype BZ1. CL 218872 exhibits anxiolytic, sedative and anticonvulsant activities. CL 218872 can be used in researches of anxiety related disorders and epilepsy.
    CL 218872
  • HY-141921S
    Dehydroepiandrosterone sulfate sodium-d6
    		Antagonist 99.61%
    Dehydroepiandrosterone sulfate sodium salt-d6 (DHEA sulfate sodium salt-d6; Prasterone sulfate sodium salt-d6) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate sodium-d<sub>6</sub>
  • 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-N2368
    Arecaidine
    		Inhibitor 99.63%
    Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine
  • HY-19371
    Lorediplon
    		Modulator 99.88%
    Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
    Lorediplon
Cat. No. Product Name / Synonyms Application Reactivity