1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

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-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[1][2].
    Etbicyphat-<sup>13</sup>C<sub>3</sub>
  • HY-W749797
    Nitrazolam
    Ligand
    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[1][2][3].
    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-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-160849
    N-Desmethyl Rilmazolam
    Inhibitor
    N-desmethyl Rilmazolam, a triazolobenzodiazepine, serves as an analytical reference standard. N-desmethyl Rilmazolam is an active metabolite derived from rilmazafone (HY-106547). N-desmethyl Rilmazolam is designed for use in research and forensic settings .
    N-Desmethyl Rilmazolam
  • 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-106917
    Lirequinil
    Agonist
    Lirequinil (Ro 41-3696) is an orally active partial agonist of the benzodiazepine (BDZ) receptor. Lirequinil has the effect of promoting sleep.
    Lirequinil
  • HY-145258
    GABAA receptor agent 6
    GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability.
    GABAA receptor agent 6
  • HY-N0067S2
    γ-Aminobutyric acid-4,4-d2
    Agonist
    γ-Aminobutyric acid-4,4-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-4,4-d<sub>2</sub>
  • HY-147421
    Xilmenolone
    Modulator
    Xilmenolone is a GABAA receptor positive allosteric modulator.
    Xilmenolone
  • HY-107994A
    Aminoxyacetic acid
    Inhibitor
    Aminooxyacetic acid (Carboxymethoxylamine) is a malate-aspartate shuttle (MAS) inhibitor. Aminooxyacetic acid also inhibits the GABA degradating enzyme GABA-T.
    Aminoxyacetic acid
  • HY-115856
    Sch 50910
    Sch 50910 is a GABA(B) receptor antagonist with some activity in inhibiting GABA(B) autoreceptors. Sch 50910 had no effect on electrically stimulated release at a concentration of 100 μM. The activity of Sch 50910 suggests that it may not have a significant role in studies of GABA(B) receptor function.
    Sch 50910
  • HY-N0659R
    Jujuboside A (Standard)
    Agonist
    Jujuboside A (Standard) is the analytical standard of Jujuboside A. This product is intended for research and analytical applications. Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, a Chinese herbal medicine used to treat insomnia and anxiety.
    Jujuboside A (Standard)
  • HY-170833
    Anticonvulsant agent 8
    Inhibitor
    Anticonvulsant agent 8 (compound D4) is an anticonvulsant agent that inhibits GABAA currents with ED50 values of 2.23 and 24.60 mg/kg in the maximum electroshock (MES) and pentylenetetrazol (PTZ) tests in mouse models, respectively.
    Anticonvulsant agent 8
Cat. No. Product Name / Synonyms Application Reactivity