1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

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-14953R
    Imepitoin (Standard)
    Agonist
    Imepitoin (Standard) is the analytical standard of Imepitoin. This product is intended for research and analytical applications. Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
    Imepitoin (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-W012123R
    3,4,5-Trimethoxycinnamic acid (Standard)
    Agonist
    3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.
    3,4,5-Trimethoxycinnamic acid (Standard)
  • HY-19945R
    DAA-1106 (Standard)
    Agonist
    DAA-1106 (Standard) is the analytical standard of DAA-1106. This product is intended for research and analytical applications. 0
    DAA-1106 (Standard)
  • 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-B0033R
    Vigabatrin hydrochloride (Standard)
    Inhibitor
    Vigabatrin (hydrochloride) (Standard) is the analytical standard of Vigabatrin (hydrochloride). This product is intended for research and analytical applications. Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
    Vigabatrin hydrochloride (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.
    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-121877R
    Valnoctamide (Standard)
    Valnoctamide (Standard) is the analytical standard of Valnoctamide. This product is intended for research and analytical applications. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors.
    Valnoctamide (Standard)
  • HY-150334
    Rilmazolam
    Rilmazolam, a triazolobenzodiazepine, is an active metabolite of Rilmazafone (HY-106547).
    Rilmazolam
  • HY-B1606
    Chlorothymol
    Activator 99.70%
    Chlothymol is a potent positive modulator of the GABAA receptor subunit LGC-37, anticonvulsant, and antibacterial agent. Chlothymol inhibits Pentylenetetrazol-induced c-fos expression. Chlothymol inhibits the growth of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) strains, including LAC, with an MIC of 32 μg/mL. Chlorothymol has protective effects against epileptic seizures in various mouse models.
    Chlorothymol
  • HY-B0007B
    (S)-Baclofen
    Agonist
    (S)-Baclofen is a selective GABAB receptor agonist with the IC50 values of 1.77 μM and 1564 μM for GABAB and GABAA, respectively.
    (S)-Baclofen
  • HY-N8472
    Chrodrimanin B
    Antagonist
    Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on?B.?mori GABAR RDL with an IC50?of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC50?of 1.66 nM.?Chrodrimanin B, a meroterpenoid, shows insecticidal activity.
    Chrodrimanin B
  • HY-B0009R
    Flumazenil (Standard)
    Antagonist
    Flumazenil (Standard) is the analytical standard of Flumazenil. This product is intended for research and analytical applications. Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
    Flumazenil (Standard)
  • HY-103530R
    CGP35348 (Standard)
    Antagonist
    CGP35348 (Standard) is the analytical standard of CGP35348. This product is intended for research and analytical applications. CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.
    CGP35348 (Standard)
  • HY-100813R
    Saclofen (Standard)
    Antagonist
    Saclofen (Standard) is the analytical standard of Saclofen.
    Saclofen (Standard)
  • HY-177552
    4''-Oxoavermectin B1a
    Ligand
    4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.
    4''-Oxoavermectin B1a
  • HY-117106
    PNU-107484A
    PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl- currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes.
    PNU-107484A
  • HY-Y1176R
    Isonipecotic acid (Standard)
    Agonist
    Isonipecotic acid is a GABAA receptor partial agonist.
    Isonipecotic acid (Standard)
  • HY-16579AR
    Etifoxine (Standard)
    Activator
    Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. 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.
    Etifoxine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity