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-131693
    γ-Acetylenic GABA
    		Inhibitor
    γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain. γ-Acetylenic GABA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    γ-Acetylenic GABA
  • HY-B0211S
    Riluzole-13C,15N2
    		99.90%
    Riluzole-13C,15N2 is the 13C and 15N labeled Riluzole[1]. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM[2][3].
    Riluzole-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • HY-100686
    U93631
    		Inhibitor 99.85%
    U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.
    U93631
  • HY-N9506
    Anisatin
    		Antagonist ≥99.0%
    Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM.
    Anisatin
  • HY-100982
    (E) -4-Hydroxycrotonic acid
    		≥98.0%
    (E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models.
    (E) -4-Hydroxycrotonic acid
  • HY-W005749
    (R)-4-Amino-3-hydroxybutyric acid
    		Agonist
    (R)-4-Amino-3-hydroxybutyric acid ((R)-GABOB) is a 4-aminobutyric acids (GABAB) agonist. (R)-4-Amino-3-hydroxybutyric acid is promising for research of nervous disorders.
    (R)-4-Amino-3-hydroxybutyric acid
  • HY-123801
    MIDD0301
    		Modulator 98.14%
    MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone (HY-B0214). MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.
    MIDD0301
  • HY-106025
    Radequinil
    		Antagonist 99.25%
    Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.
    Radequinil
  • HY-103527
    RuBi-GABA
    RuBi-GABA is a new ruthenium-based caged GABA compound. RuBi-GABA photocleaves and releases GABA after being excited with visible wavelengths. RuBi-GABA produces gaba receptor-mediated currents.
    RuBi-GABA
  • HY-P5964A
    K1 peptide TFA
    		Ligand 98.22%
    K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP).
    K1 peptide TFA
  • HY-110234
    Topiramate D12
    		Activator 99.90%
    Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate 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 D12
  • HY-101060
    FGIN 1-43
    		Inhibitor 98.96%
    FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN 1-43
  • HY-101060
    FGIN 1-43
    		Activator 98.96%
    FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN 1-43
  • HY-100799
    ZAPA sulfate
    		Agonist 99.25%
    ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM.
    ZAPA sulfate
  • HY-108034
    GET73
    		98.69%
    GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.
    GET73
  • HY-A0198
    Adinazolam
    		Agonist ≥99.0%
    Adinazolam (U 41123) is a benzodiazepine agonist. Adinazolam, a triazolobenzodiazepine, has dual anxiolytic and antidepressant activities.
    Adinazolam
  • HY-101359
    TPMPA
    		Antagonist 98.1%
    TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells.
    TPMPA
  • HY-105272
    Loreclezole
    		Agonist 99.68%
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
    Loreclezole
  • HY-10061
    Lesogaberan
    		Agonist
    Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan
  • HY-133486
    GABAA receptor agent 1
    		98.93%
    GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity.
    GABAA receptor agent 1
Cat. No. Product Name / Synonyms Application Reactivity