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-174147
    GABAB receptor antagonist 4
    		Antagonist
    GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases.
    GABAB receptor antagonist 4
  • HY-101808
    Doxefazepam
    		99.96%
    Doxefazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsan and skeletal muscle relaxant properties.
    Doxefazepam
  • HY-19308
    RWJ-51204
    		Agonist
    RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
    RWJ-51204
  • HY-101583
    NEO 376
    		Modulator 99.23%
    NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
    NEO 376
  • HY-118625
    CP-457920
    		Inhibitor
    CP-457920 (Compound 21) is a GABA receptor inhibitor (Ki ≈ 1 ng/mL). CP-457920 can be used in research on neurological diseases such as Alzheimer's disease.
    CP-457920
  • HY-114883
    Homocarnosine
    Homocarnosine is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects.Homocarnosine has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.
    Homocarnosine
  • HY-B0765R
    Dehydroepiandrosterone sulfate sodium (Standard)
    		Antagonist
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate sodium (Standard)
  • HY-170771
    α5-GABAA receptor modulator 1
    		Modulator
    α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABAA receptor, suitable for research into central nervous system (CNS) disorders.
    α5-GABAA receptor modulator 1
  • HY-107482A
    Picamilon sodium
    		Agonist
    Picamilon sodium is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon sodium improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.
    Picamilon sodium
  • HY-175190
    GABA receptor antagonist 2
    		Antagonist
    GABA receptor antagonist 2 (Compound IId) is a GABA receptor antagonist with a LC50 of 0.0735 μg/mL for Plutella xylostella (P. xylostella). GABA receptor antagonist 2 has significant insecticidal activities against P. xylostella and its resistant strain, and Spodoptera frugiperda, and Chilo suppressalis. GABA receptor antagonist 2 binds the GABA receptor at the site of Drosophila RdlG335. GABA receptor antagonist 2 can be used to manage resistant pest populations.
    GABA receptor antagonist 2
  • HY-161784
    GABAA receptor modulator-5
    		Modulator
    GABAA receptor modulator-5 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC50 of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression.
    GABAA receptor modulator-5
  • HY-178782
    GABAA receptor modulator-11
    		Modulator
    GABAA receptor modulator-11 (Compound 4) is a GABAA receptor modulator. GABAA receptor modulator-11 inhibits anesthetic-induced desensitization of GABAA α1β3γ2 and α1β3 receptors, with IC50 values of 5.1 μM and 3.1 μM, respectively. GABAA receptor modulator-11 can be used for research on central nervous system diseases.
    GABAA receptor modulator-11
  • HY-100783B
    Bicuculline methobromide
    		Antagonist
    Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders.
    Bicuculline methobromide
  • HY-113320R
    Etiocholanolone (Standard)
    		Modulator
    Cimbuterol (Standard) is the analytical standard of Cimbuterol. This product is intended for research and analytical applications. Cimbuterol is a β-adrenergic receptor agonist.
    Etiocholanolone (Standard)
  • HY-134912
    CMPPE
    		Modulator
    CMPPE is a GABAB receptor positive allosteric modulator (PAM) that inhibits alcohol self-administration and reinstatement behavior in rats.
    CMPPE
  • HY-W707498
    Baclofen-d4-1
    Baclofen-d4-1 is the deuterium labeled Baclofen (HY-B0007). 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>-1
  • HY-130670
    CGP 54626
    		Modulator
    CGP 54626 is a GABAB receptor modulator, which is essential in the central and peripheral nervous systems. It is used as a tool to identify and characterize GABAB receptor agonists and antagonists, which will aid in the development of drugs targeting diseases related to these systems. This discovery involves purified GABAB receptors, receptor proteins and their encoding nucleic acids, facilitating the study of new members of the GABAB receptor family through DNA cloning technology and sequence-derived probes.
    CGP 54626
  • HY-117560
    PWZ-029
    		Agonist
    PWZ-029 is a selective inverse agonist for 5 GABAA receptors. PWZ-029 is a benzodiazepine site ligand. PWZ-029 shows a weak but significant partial agonistic effect at 1- and 3-containing receptors. PWZ-029 significantly increases retention session latency in mouse fibroblast cells. PWZ-029 can improve object recognition in normal and scopolamine-treated rat model.
    PWZ-029
  • HY-147657
    GABAA receptor modulator-2
    		Modulator
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety.
    GABAA receptor modulator-2
  • HY-155498
    TETS-4-Methylaniline
    		Inhibitor
    TETS-4-Methylaniline (compound 2k) is a hapten. TETS-4-Methylaniline conjugates to the carrier protein via using either diazotization or glutaraldehyde methods.
    TETS-4-Methylaniline
Cat. No. Product Name / Synonyms Application Reactivity