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-120192
    CGP 62349
    		Antagonist
    CGP 62349 is a selective and orally active GABAB receptor antagonist that improves cognitive performance in multiple learning paradigms.
    CGP 62349
  • HY-10232R
    THIP (Standard)
    		Antagonist
    THIP (Standard) is the analytical standard of THIP. This product is intended for research and analytical applications. THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders[1][2][3].
    THIP (Standard)
  • HY-B0122SS1
    Topiramate-13C6-1
    		Activator
    Topiramate-13C6-1 (McN 4853-13C6-1; RWJ 17021-13C6-1) is 13C-labeled Topiramate (HY-B0122).
    Topiramate-<sup>13</sup>C<sub>6</sub>-1
  • HY-168363
    Ciclotizolam
    		Ligand
    Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats.
    Ciclotizolam
  • HY-16579AS2
    Etifoxine-d5
    		Activator
    Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].
    Etifoxine-d<sub>5</sub>
  • HY-103476R
    Ro15-4513 (Standard)
    		Antagonist
    Ro15-4513 (Standard) is the analytical standard of Ro15-4513. This product is intended for research and analytical applications. Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR)[1]. Ro15-4513 is a potent ethanol antagonist[2]. Ro15-4513 has anti-anxiety effect[3]. 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 (Standard)
  • HY-129090
    CGS-​9895
    		Antagonist
    CGS-​9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors.
    CGS-​9895
  • HY-123426
    JY-XHe-053
    		Agonist
    JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors.
    JY-XHe-053
  • HY-19082
    Y-23684
    		Agonist
    Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders.
    Y-23684
  • HY-117257
    PF-0713
    		Agonist
    PF 0713 is a GABAA receptor agonist..
    PF-0713
  • HY-105272R
    Loreclezole (Standard)
    		Agonist
    Loreclezole (Standard) is the analytical standard of Loreclezole. This product is intended for research and analytical applications. Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors[1][2].
    Loreclezole (Standard)
  • HY-121393
    Imidazenil
    		Modulator 98.95%
    Imidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
    Imidazenil
  • HY-B0696S
    Tiagabine-d6
    		Inhibitor
    Tiagabine-d6 (NO050328-d6) is deuterium labeled Tiagabine. Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
    Tiagabine-d<sub>6</sub>
  • HY-101392A
    Harmane hydrochloride
    		Inhibitor
    Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane hydrochloride
  • HY-N0301R
    Thiocolchicoside (Standard)
    		Antagonist
    Thiocolchicoside (Standard) is the analytical standard of Thiocolchicoside. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B1833S
    Afloqualone-d7
    		Agonist
    Afloqualone-d7 (HQ-495-d7) is deuterium labeled Afloqualone. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome.
    Afloqualone-d<sub>7</sub>
  • HY-Y1683R
    DL-Menthol (Standard)
    		Activator
    DL-Menthol (Standard) is the analytical standard of DL-Menthol. This product is intended for research and analytical applications. DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor.
    DL-Menthol (Standard)
  • HY-100991R
    FG 7142 (Standard)
    		Inhibitor
    FG 7142 (Standard) is the analytical standard of FG 7142. This product is intended for research and analytical applications. FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex[1].
    FG 7142 (Standard)
  • HY-W681659
    Flutoprazepam
    		Inhibitor
    Flutoprazepam (KB-509), a benzodiazepine drug, possesses anticonflict effect. Flutoprazepam (KB-509) prevents maximal electroshock, pentetrazol, and strychnine-induced convulsions in mice.
    Flutoprazepam
  • HY-150334
    Rilmazolam
    Rilmazolam, a triazolobenzodiazepine, is an active metabolite of Rilmazafone (HY-106547).
    Rilmazolam
Cat. No. Product Name / Synonyms Application Reactivity