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-118635
    Cyprodenate
    		Antagonist ≥98.0%
    Cyprodenate (Actebral) is an orally active psychotonic brain activator. Cyprodenate can be used for the research of metabolism.
    Cyprodenate
  • HY-133594
    Sandaracopimaric acid
    		Inhibitor 98.86%
    Sandaracopimaric acid is a diterpenoid with anti-inflammatory effect. Sandaracopimaric acid reduces the contraction of phenylephrine-induced pulmonary arteries with an EC50 of 43.93 μM.
    Sandaracopimaric acid
  • HY-138014
    Cinazepam
    		Agonist
    Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.
    Cinazepam
  • HY-100140
    Pipequaline
    		Agonist 99.93%
    Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline
  • HY-11048
    NS11394
    		Modulator 99.77%
    NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
    NS11394
  • HY-B0122R
    Topiramate (Standard)
    		Activator
    Topiramate (Standard) is the analytical standard of Topiramate. This product is intended for research and analytical applications. Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
    Topiramate (Standard)
  • HY-101639
    CP-409092
    		Agonist
    CP-409092 is a partial agonist of GABAA receptor, with anti-anxiety activity.
    CP-409092
  • HY-122489A
    (S)-Laudanosine
    		Control 99.95%
    (S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM).
    (S)-Laudanosine
  • HY-159504
    Pregabalinum naproxencarbilum
    Pregabalinum naproxencarbilum (Pregabalin naproxencarbil) is a gabamimetic (GABA), analgesic compound.
    Pregabalinum naproxencarbilum
  • HY-155238
    E2730
    		Inhibitor
    E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg).
    E2730
  • HY-107323
    Bentazepam
    		Ligand
    Bentazepam (Thiadipone) is a compound with short-action anxiolytic effect. Bentazepam shows anticonvulsant and sedative properties. Bentazepam can be used for the research of depressive disorder and anxiety.
    Bentazepam
  • HY-14735
    Arbaclofen placarbil
    		Agonist
    Arbaclofen placarbil is a novel transported proagent of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist
    Arbaclofen placarbil
  • HY-17030S
    Acamprosate-d3 calcium
    		Agonist ≥98.0%
    Acamprosate-d3 (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems.
    Acamprosate-d<sub>3</sub> calcium
  • HY-B0339S
    Primidone-d5
    		Antagonist ≥99.00%
    Primidone-d5 is the deuterium labeled Primidone. 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-d<sub>5</sub>
  • HY-B0007S
    Baclofen-d4
    		Agonist 99.98%
    Baclofen-d4 is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
    Baclofen-d<sub>4</sub>
  • HY-110233S
    Acamprosate-d6 calcium
    		Agonist
    Acamprosate-d6 (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium (Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems.
    Acamprosate-d<sub>6</sub> calcium
  • HY-W013150S
    Alpidem-d14
    Alpidem-d14 is the deuterium labeled Alpidem.
    Alpidem-d<sub>14</sub>
  • HY-103501
    SB-205384
    		Modulator
    SB-205384 is a GABAA receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist.
    SB-205384
  • HY-103510
    TB-21007
    		Inhibitor 99.7%
    TB-21007 is a selective and brain penetrant α5 subunit-containing GABAA receptor inverse agonist with Kis of 1.6 nM, 20 nM, 16 nM, and 20 nM for α5, α1, α2 and α3 subtypes, respectively. TB-21007 enhances cognition in rats.
    TB-21007
  • HY-114300
    DSP-0565
    		Agonist
    DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin.
    DSP-0565
Cat. No. Product Name / Synonyms Application Reactivity