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-W707528
    Propofol-d14
    Propofol-d14 (2,6-Diisopropylphenol-d14) is the deuterium labeled Propofol (HY-B0649). Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
    Propofol-d<sub>14</sub>
  • 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-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
  • HY-147735
    GABAA receptor agonist 1
    		Agonist
    GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression.
    GABAA receptor agonist 1
  • HY-103496
    U-90042
    		Agonist
    U-90042 is a gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with Ki values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent.
    U-90042
  • HY-105272A
    Loreclezole hydrochloride
    		Agonist
    Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
    Loreclezole hydrochloride
  • HY-113726
    Nerisopam
    		Agonist
    Nerisopam is an orally active gamma-aminobutyric acid (GABA) receptor agonist. Nerisopam is an anxiolytic and antipsychotic homophthalazine. Nerisopam induces rapid, intense expression of Fos-like immunoreactivity in the rostral, dorsomedial and lateral parts of the striatum in the rat.
    Nerisopam
  • HY-19266
    RO-488684
    		Agonist
    RO-488684 is a benzodiazepine receptor agonist. RO-488684 can be used for research on sleep and conscious sedation.
    RO-488684
  • HY-123525
    COR628
    COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration.
    COR628
  • HY-N2079R
    (-)-Securinine (Standard)
    		Antagonist
    (-)-Securinine (Standard) is the analytical standard of (-)-Securinine. This product is intended for research and analytical applications. (-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
    (-)-Securinine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity