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-103668AR
    SSD114 hydrochloride (Standard)
    Agonist
    SSD114 hydrochloride (Standard) is the analytical standard of SSD114 hydrochloride (HY-103668A). This product is intended for research and analytical applications. SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
    SSD114 hydrochloride (Standard)
  • HY-100228AR
    SKF89976A hydrochloride (Standard)
    Inhibitor
    SKF89976A (hydrochloride) (Standard) is the analytical standard of SKF89976A (hydrochloride) (HY-100228A). This product is intended for research and analytical applications. SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
    SKF89976A hydrochloride (Standard)
  • HY-B1833R
    Afloqualone (Standard)
    Agonist
    Afloqualone (Standard) is the analytical standard of Afloqualone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-17599R
    Piperazine citrate (Standard)
    Agonist
    Piperazine (citrate) (Standard) is the analytical standard of Piperazine (citrate). This product is intended for research and analytical applications. Piperazine (1,4-Diazacyclohexane) citrate is a gamma-aminobutyric acid (GABA) agonist. Piperazine citrate is a vital building block and is an essential core in numerous marketed agents with diverse pharmacological activities.
    Piperazine citrate (Standard)
  • HY-171471
    SKF 10810
    Antagonist
    SKF 10810 is a GABAA receptor antagonist with an EC50 of 4.3 μM. By blocking GABAergic inhibition of the brain's reward pathways, SKF 10810 may exert antidepressant effects. SKF 10810 can be used for research in neurological disorders.
    SKF 10810
  • HY-N9407
    Guvacine ethyl ester
    Guvacine ethyl ester (3.1b) is an alkaloid that can be found in betel nut. Guvacine ethyl ester can be used in the synthesis of GABA uptake inhibitor.
    Guvacine ethyl ester
  • HY-101207
    NCS-382
    Antagonist
    NCS-382 is a potent GABA receptor antagonist and also a GHBR receptor antagonist. NCS-382 has anticonvulsant and antisedative activity. NCS-382 is used in the related research of hereditary nervous system diseases.
    NCS-382
  • HY-101414R
    L-DABA (Standard)
    Inhibitor
    L-DABA (Standard) is the analytical standard of L-DABA. This product is intended for research and analytical applications. L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
    L-DABA (Standard)
  • HY-A0198A
    Adinazolam mesylate
    Agonist
    Adinazolam (U 41123F) mesylate is a triazolobenzodiazepine. Adinazolam mesylate binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam mesylate has dual anxiolytic and antidepressant activities.
    Adinazolam mesylate
  • HY-111136
    BL-1020 mesylate
    Agonist
    BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate.
    BL-1020 mesylate
  • HY-14856A
    iso-Atagabalin hydrochloride
    Agonist
    iso-Atagabalin (iso-PD 0200390) hydrochloride is a stereoisomer of Atagabalin (HY-14856). Atagabalin is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety effect.
    iso-Atagabalin hydrochloride
  • HY-129408
    SGE-516
    Modulator
    SGE-516 is a neuroactive steroid that is a potent positive allosteric modulator of synaptic and extra-synaptic GABAA receptors. SGE-516 has anticonvulsant activity.
    SGE-516
  • HY-103504R
    (S)-SNAP5114 (Standard)
    Inhibitor
    (S)-SNAP5114 (Standard) is the analytical standard of (S)-SNAP5114 (HY-103504). This product is intended for research and analytical applications. (S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant agent.
    (S)-SNAP5114 (Standard)
  • HY-183910
    Pitrazepin
    Antagonist
    Pitrazepin is a GABAA receptor antagonist and glycine receptor antagonist. Pitrazepin blocks synaptic GABA action, induces neuronal bursting and reduces inhibitory postsynaptic potentials. Pitrazepin can be used in research on depression and psychosis.
    Pitrazepin
  • HY-100799R
    ZAPA sulfate (Standard)
    Agonist
    ZAPA (sulfate) (Standard) is the analytical standard of ZAPA (sulfate) (HY-100799). This product is intended for research and analytical applications. ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM.
    ZAPA sulfate (Standard)
  • HY-10233R
    Gaboxadol hydrochloride (Standard)
    Modulator
    Gaboxadol (hydrochloride) (Standard) is the analytical standard of Gaboxadol (hydrochloride). This product is intended for research and analytical applications. Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.
    Gaboxadol hydrochloride (Standard)
  • HY-N15001
    Gabaculine
    Inhibitor
    Gabaculine is an amino acid neurotoxin and blood-brain barrier-permeable GABA transaminase inhibitor, with an IC50 of 1 μM in beef and Pseudomonas ovalis. Gabaculine elevates endogenous synaptic and brain GABA levels and enhances GABA activity. Gabaculine induces sedation, hypothermia, loss of righting reflex, and prevents convulsions in mice. Gabaculine is applicable to research related to neurological disorders.
    Gabaculine
  • HY-103506R
    NNC-711 (Standard)
    Inhibitor
    NNC-711 (Standard) is the analytical standard of NNC-711 (HY-103506). This product is intended for research and analytical applications. NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC50 values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity.
    NNC-711 (Standard)
  • HY-16579R
    Etifoxine hydrochloride (Standard)
    Activator
    Etifoxine (hydrochloride) (Standard) is the analytical standard of Etifoxine (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-106437
    ELB-139
    Agonist
    ELB-139 is a progesterone analogue. ELB-139 is a GABAA receptor partial agonist. ELB-139 has anxiolytic and anticonvulsant activity. ELB-139 induces increase of extracellular 5-HT in the striatum and the medial prefrontal cortex of rats.
    ELB-139
Cat. No. Product Name / Synonyms Application Reactivity