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-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-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)
  • HY-103532
    CGP46381
    		Antagonist
    CGP 46381 is an orally active GABAB receptor antagonist with IC50 of 4.9 μM. CGP 46381 blocks the neuronal depression induced by iontophoretically applied baclofen (HY-B0007) .
    CGP46381
  • HY-B0822S1
    Fipronil-13C6
    		Antagonist
    Fipronil-13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-<sup>13</sup>C<sub>6</sub>
  • HY-Y1176S
    Isonipecotic acid-d9
    Isonipecotic acid-d9 is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].
    Isonipecotic acid-d<sub>9</sub>
  • HY-105115
    Abecarnil
    		Modulator
    Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
    Abecarnil
  • HY-P5964
    K1 peptide
    		Ligand
    K1 peptide is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP).
    K1 peptide
  • HY-119404
    Diproqualone
    		Agonist
    diproqualone is methaqualone analogous with sedative, anxiolytic, anti-inflammatory and analgesic properties.
    Diproqualone
  • HY-W751152
    α,β-Thujone
    		Inhibitor
    α,β-Thujone is a component of the essential oils of some plants. α,β-Thujone causes cancers in male rats and induces seizures in the highest doses.
    α,β-Thujone
  • HY-129451
    HIE-124
    		Inhibitor
    HIE-124 is a potent ultra-short acting hypnotic that exhibits a rapid onset of action and a shorter duration of action with no acute tolerance or noticeable side effects. HIE-124 is promising for research of preanesthetic medication and anesthesia inducer.
    HIE-124
  • HY-B0007R
    Baclofen (Standard)
    		Agonist
    Baclofen (Standard) is the analytical standard of Baclofen. This product is intended for research and analytical applications. 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 (Standard)
  • HY-112426
    LAU159
    		Antagonist
    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
    LAU159
  • HY-P10898
    GeX-2
    		Activator
    GeX-2 is a truncated analogue of αO-conotoxin. GeX-2 activates GABAB receptor. GeX-2 inhibits α9α10 nAChR and CaV2.2 channels. GeX-2 alleviates pain in the rat model of chronic constriction injury.
    GeX-2
  • HY-100291
    SX-3228
    		Agonist
    SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.
    SX-3228
  • HY-B0649S
    Propofol-d17
    		Activator
    Propofol-d17 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties[1].
    Propofol-d<sub>17</sub>
  • HY-B0822R
    Fipronil (Standard)
    		Antagonist
    Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
    Fipronil (Standard)
Cat. No. Product Name / Synonyms Application Reactivity