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-N2160
    6'''-Feruloylspinosin
    		99.65%
    6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
    6'''-Feruloylspinosin
  • 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-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
  • 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-B1803A
    Tracazolate hydrochloride
    		Modulator 99.24%
    Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
    Tracazolate hydrochloride
  • HY-107489
    RO 4938581
    		Antagonist 99.78%
    RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
    RO 4938581
  • HY-N0301
    Thiocolchicoside
    		Antagonist 99.54%
    Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
    Thiocolchicoside
  • HY-108690
    Fluxametamide
    		Antagonist 99.45%
    Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
    Fluxametamide
  • HY-13694S1
    Methionine-d4
    		Activator ≥98.0%
    Methionine-d4 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>4</sub>
  • 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-N2368A
    Arecaidine hydrochloride
    		Inhibitor 98.00%
    Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine hydrochloride
  • HY-15377
    DL-Gabaculine hydrochloride
    		Inhibitor 99.90%
    DL-Gabaculine hydrochloride is a neurotoxin that irreversibly inhibits bacterial pyridoxal phosphate linked γ-aminobutyric acid-α-ketoglutaric acid transaminase with a Ki of 2.86 μM.
    DL-Gabaculine hydrochloride
  • HY-116622
    α5IA
    		Agonist
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential.
    α5IA
  • HY-B0135R
    Furosemide (Standard)
    		Antagonist
    Furosemide (Standard) is the analytical standard of Furosemide. This product is intended for research and analytical applications. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
    Furosemide (Standard)
  • HY-N6628
    6,2'-Dihydroxyflavone
    		Antagonist 99.54%
    6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
    6,2'-Dihydroxyflavone
  • 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-107994A
    Aminoxyacetic acid
    		Inhibitor
    Aminooxyacetic acid (Carboxymethoxylamine) is a malate-aspartate shuttle (MAS) inhibitor. Aminooxyacetic acid also inhibits the GABA degradating enzyme GABA-T.
    Aminoxyacetic acid
  • 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-B0339R
    Primidone (Standard)
    		Antagonist
    Primidone (Standard) is the analytical standard of Primidone. This product is intended for research and analytical applications. Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.
    Primidone (Standard)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity