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-14840
    Phenylpiracetam
    		Activator 99.91%
    Phenylpiracetam(Phenotropyl; Phenotropil) is a phenylated derivative of the nootropic drug piracetam.
    Phenylpiracetam
  • HY-103509
    NNC 05-2090 hydrochloride
    		Inhibitor 99.09%
    NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.
    NNC 05-2090 hydrochloride
  • HY-114883A
    Homocarnosine TFA
    		99.67%
    Homocarnosine TFA is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine TFA is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects. Homocarnosine TFA has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.
    Homocarnosine TFA
  • HY-123489
    3α,21-Dihydroxy-5α-pregnan-20-one
    		Agonist ≥98.0%
    3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
    3α,21-Dihydroxy-5α-pregnan-20-one
  • HY-121618
    α-Thujone
    		Modulator 98.07%
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and can cross the blood-brain barrier.
    α-Thujone
  • HY-16579A
    Etifoxine
    		Activator 99.96%
    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
  • HY-101869
    MK-0343
    		Agonist 99.31%
    MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.
    MK-0343
  • HY-B1833
    Afloqualone
    		Agonist 99.94%
    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
  • HY-119687
    Bifenazate
    		Agonist 99.89%
    Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor. Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III.
    Bifenazate
  • HY-132806
    Alogabat
    		Agonist 99.93%
    Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction.
    Alogabat
  • HY-B0353
    Chlormezanone
    		99.80%
    Chlormezanone resembles benzodiazepine. The action of Chlormezanone is similar to benzodiazepine-type agents. Chlormezanone is used as an anxiolytic and a muscle relaxant.
    Chlormezanone
  • HY-153584
    MRK-898
    		Modulator 99.48%
    MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s).
    MRK-898
  • HY-100809
    Guvacine hydrochloride
    		Inhibitor 99.73%
    Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
    Guvacine hydrochloride
  • HY-121599
    CGP 36742
    		Antagonist ≥98.0%
    CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a blood-brain barrier (BBB) penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study.
    CGP 36742
  • HY-113346
    Tetrahydrodeoxycorticosterone
    		Agonist 99.45%
    Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.
    Tetrahydrodeoxycorticosterone
  • HY-Y1683
    DL-Menthol
    		Activator ≥98.0%
    DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production.
    DL-Menthol
  • HY-W012738S
    DL-Pyroglutamic acid-d5
    		99.21%
    DL-Pyroglutamic acid-d5 is the deuterium labeled DL-Pyroglutamic acid[1].
    DL-Pyroglutamic acid-d<sub>5</sub>
  • HY-100936
    Etazolate hydrochloride
    		Modulator 98.00%
    Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
    Etazolate hydrochloride
  • HY-139116
    Piperidine-4-sulfonic acid
    		99.95%
    Piperidine-4-sulfonic acid is a potent GABA agonist with an IC50 of 0.034 μM for the inhibition of the binding of H-GABA.
    Piperidine-4-sulfonic acid
  • HY-139427
    3-Methylglutaconic acid
    		99.60%
    3-Methylglutaconic acid is the major metabolites accumulating in 3-Methylglutaconic aciduria (MGTA). 3-Methylglutaconic acid can induce lipid oxidative damage and protein oxidative. 3-Methylglutaconic acid decreases the non-enzymatic antioxidant defenses in cerebral cortex supernatants to elicit oxidative stress in the cerebral cortex. 3-Methylglutaconic acid can be used for brain damage disease research.
    3-Methylglutaconic acid
Cat. No. Product Name / Synonyms Application Reactivity