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-103498
    Org20599
    		Antagonist
    Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM.
    Org20599
  • HY-182271
    GPR61 Inverse agonist 3
    		Inhibitor
    GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia.
    GPR61 Inverse agonist 3
  • HY-B0696B
    Tiagabine hydrochloride hydrate
    		Inhibitor
    Tiagabine (NO050328; NO328; TGB) hydrochloride hydrate is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride hydrate exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride hydrate is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
    Tiagabine hydrochloride hydrate
  • HY-W754627
    Clazolam
    		Modulator
    Clazolam (Isoquinazepon; SAH-1123) is a GABA Receptor modulator. Clazolam can be used in research on neurological diseases.
    Clazolam
  • HY-106044
    Etazolate
    		Modulator
    Etazolate (SQ 64442) is a α-secretase activator, selective PDE4 inhibitor, selective GABAA receptor modulator. Etazolate reduces IL-1β levels Etazolate exerts a dose-dependent anti-inflammatory and anti-œdematous effect accompanied by lasting memory improvement. Etazolate produces an antidepressant-like effect.
    Etazolate
  • HY-114040
    NO-711
    		Inhibitor
    NO-711 (NNC-711) free acid is a novel potent and selective inhibitor of γ-aminobutyric acid uptake. NO-711 inhibits synaptosomal (IC50 = 47 nM), neuronal (IC50 = 1238 nM) and glial (IC50 = 636 nM) GABA uptake in vitro.
    NO-711
  • HY-181961
    SR-THAP
    		Inhibitor
    SR-THAP is a γ-aminobutyric acid transporter 3 (GAT3) inhibitor with an IC50 of 4.9 μM, and exhibits 42-fold and 23-fold selectivity over GAT1 and GlyT1, respectively. SR-THAP inhibits GABA uptake in mammalian cells. SR-THAP is applicable to the research of epilepsy, Alzheimer's disease and ischemic stroke.
    SR-THAP
  • HY-139145S
    Etbicyphat-13C3
    Etbicyphat-13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors.
    Etbicyphat-<sup>13</sup>C<sub>3</sub>
  • HY-W749797
    Nitrazolam
    		Ligand 99.9%
    Nitrazolam is a benzodiazepine compound, that may exhibit CNS depressant properties as traditional benzodiazepines, including sedation, hypnosis, anxiolysis, and anticonvulsant effects, by acting on GABA receptors.
    Nitrazolam
  • HY-B0033S
    Vigabatrin-13C,d2 hydrochloride
    		Inhibitor
    Vigabatrin-13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). 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-<sup>13</sup>C,d<sub>2</sub> hydrochloride
  • HY-100924
    β-CCB
    β-CCB is a ligand for benzodiazepine receptor, which inhibits the binding of [3H]flunitrazepam and ethyl (3-[3H]carboline-3-carboxylate to benzodiazepine receptors, with Ki of 3-4 nM. β-CCB exhibits proconvulsant and anxiogenic effects.
    β-CCB
  • HY-106965
    Org 21465
    		Inhibitor
    Org 21465 is an agent that can relieve pain. Org 21465 causes no cardiovascular or respiratory depression. Org 21465 can inhibit GABAA receptor in vivo.
    Org 21465
  • HY-108689R
    Broflanilide (Standard)
    		Antagonist
    Broflanilide (Standard) is the analytical standard of Broflanilide. This product is intended for research and analytical applications. Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
    Broflanilide (Standard)
  • HY-116197
    CGP44532
    		Agonist
    CGP44532 is a GABAB receptor agonist with a pEC50 (geometric mean of the half-maximal effective concentration) value of 5.63 μM.
    CGP44532
  • HY-W707528
    Propofol-d14
    Propofol-d14 (2,6-Diisopropylphenol-d14) is the deuterium labeled Propofol (HY-B0649). Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
    Propofol-d<sub>14</sub>
  • HY-156339
    GABA receptor Antagonist 1
    		Antagonist
    GABA receptor Antagonist 1 (compound 7w) inhibits Px RDL1 GABAR with an IC50 value of 7.08 nmol/L. GABA receptor Antagonist 1 shows insecticide activity against P. xylostella, S. frugiperda, S. exigua, and S. litura, with LC50 of 0.09, 0.84, 0.87, and 0.68 mg/L respectively. GABA receptor Antagonist 1 shows a medium toxicity to honeybee (48 h, ID50 = 2.22 μg/adult), and low toxicity to zebrafish (LC50: 42.4 mg/L).
    GABA receptor Antagonist 1
  • HY-129464
    NO-711ME
    		Inhibitor
    NO-711ME is a prodrug of NO-711. NO-711 is a potent and selective GABA uptake inhibitor.
    NO-711ME
  • HY-119256
    COR627
    COR627 is a GABA receptor positive allosteric modulator with the ability to enhance GABA activity. COR627 exhibits effects on GABA and baclofen stimulation in rat cortical membranes and can increase its affinity for GABA(B) receptors. In vivo experiments have shown that COR627 can enhance the sedative/hypnotic effects of baclofen at pretreatment ineffective doses.
    COR627
  • HY-123478
    Fengabine
    		Agonist
    Fengabine is a GABAergic antidepressant agent. Fengabine can be used for the research of depression.
    Fengabine
  • HY-W436366
    SSR180575
    		Ligand
    SSR180575 is a specific and potent peripheral benzodiazepine receptor ligand. SSR180575 irreversibly and specifically binds with high affinity on rat heart mitochondria (Kd = 1.95 nM). SSR180575 can be used in the research of cardiovascular diseases.
    SSR180575
Cat. No. Product Name / Synonyms Application Reactivity