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-119591
    BPDBA
    		Inhibitor 99.40%
    BPDBA is a selective and noncompetitive betaine/GABA transporter (BGT-1) inhibitor with IC50s of 20 μM and 35 μM against human BGT-1 and mouse GAT2, respectively.
    BPDBA
  • HY-101378
    CGP 54626 hydrochloride
    		Antagonist 99.76%
    CGP 54626 (hydrochloride) is a selective antagonist of GABAB receptor with an IC50 value of 4 nM. CGP 54626 (hydrochloride) can be used to investigate the role of GABAB receptors in neurological signaling.
    CGP 54626 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-B0504R
    Creatinine (Standard)
    		Modulator
    Creatinine (Standard) is the analytical standard of Creatinine. This product is intended for research and analytical applications. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.
    Creatinine (Standard)
  • HY-16716
    Basmisanil
    		Inhibitor 99.40%
    Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.
    Basmisanil
  • HY-B0007C
    Baclofen hydrochloride
    		Agonist 99.78%
    Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research.
    Baclofen hydrochloride
  • HY-B0355
    Ginkgolide A
    		Antagonist 99.07%
    Ginkgolide A (BN-52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist.
    Ginkgolide A
  • HY-103519
    rac-BHFF
    		Activator 98.25%
    rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor.
    rac-BHFF
  • HY-116564
    Lotilaner
    		Antagonist 99.84%
    Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor.
    Lotilaner
  • HY-139427
    3-Methylglutaconic acid
    		99.75%
    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
  • HY-N2096
    Kavain
    		Activator 99.89%
    Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
    Kavain
  • HY-N0067S1
    γ-Aminobutyric acid-d2
    		Agonist 99.95%
    γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
    γ-Aminobutyric acid-d<sub>2</sub>
  • HY-103509
    NNC 05-2090 hydrochloride
    		Inhibitor 98.53%
    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-100809
    Guvacine hydrochloride
    		Inhibitor 99.93%
    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-N6084
    Humulone
    		Activator 99.46%
    Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
    Humulone
  • 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 brain-penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study.
    CGP 36742
  • HY-B0135A
    Furosemide sodium
    		Antagonist 99.87%
    Furosemide sodium is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
    Furosemide sodium
  • HY-B0696
    Tiagabine
    		Inhibitor 98.49%
    Tiagabine (NO050328; NO328; TGB) 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 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 is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
    Tiagabine
  • HY-W015595
    L-Allylglycine hydrochloride
    		Antagonist 98.0%
    L-Allylglycine (L-2-Allylglycine) hydrochloride is an amino acid derivative. L-Allylglycine hydrochloride is an inhibitor for glutamate decarboxylase (GAD) that reduces the GABA biosynthesis in the brain. L-Allylglycine hydrochloride exhibits convulsant activity.
    L-Allylglycine hydrochloride
  • HY-B0340
    Nefiracetam
    		Activator 99.87%
    Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.
    Nefiracetam
Cat. No. Product Name / Synonyms Application Reactivity