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-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. Isonipecotic acid is a GABAA receptor partial agonist.
    Isonipecotic acid-d<sub>9</sub>
  • HY-105115
    Abecarnil
    		Modulator 99.38%
    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-172588
    GABAA receptor modulator-7
    		Modulator
    GABAA receptor modulator-7 (compound 1m), a spiro-Barbiturate, is a GABAA receptor modulator. GABAA receptor modulator-7 reverses the action of anesthetics without affecting GABA-induced desensitization and can be used for study of antiepileptics and anxiolytics.
    GABAA receptor modulator-7
  • HY-N16476
    Spinosyn J
    		Modulator
    Spinosyn J is a non-competitive insect nicotinic acetylcholine receptor (nAChR) and γ-aminobutyric acid (GABA) receptor modulator with insecticidal activity. Spinosyn J is promising for research of agricultural pests.
    Spinosyn J
  • 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-W740245
    Arecaidine-d5 hydrobromide
    Arecaidine-d5 hydrobromide is the deuterium labeled Arecaidine hydrobromide (HY-N2368B). Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine-d<sub>5</sub> hydrobromide
  • 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 98.90%
    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.
    Propofol-d<sub>17</sub>
  • HY-N16421
    Leporin A
    		Ligand
    Leporin A is an insecticide. Leporin A binds to GABA receptors or sodium channels to disrupt neurotransmission.
    Leporin A
  • HY-118096
    AHN 070
    		Ligand
    AHN 070 is an irreversible peripheral benzodiazepine receptor (PBR) ligand. AHN 070 can bind to PBR with nanomolar affinity and is pH-dependent. AHN 070 can be used for studying the structure and function of PBR.
    AHN 070
  • HY-U00315S
    Gidazepam-d5
    		Antagonist
    Gidazepam-d5 is a deuterium labeled Gidazepam. Gidazepam is an agonist of GABA receptor channels (GABA RCs), and has anticonvulsant effect.
    Gidazepam-d<sub>5</sub>
  • HY-175263
    Aminochalcone 4AAF
    Aminochalcone 4AAF is a neuroprotective agent that exerts anxiolytic effects through GABAA and 5-HT receptors. Aminochalcone 4AAF has high selectivity for 5-HT3A and 5-HT2C receptors, and stimulates allosteric behavior toward the 5-HT2A receptor. Aminochalcone 4AAF shows hypoglycemic effects and reduces the level of ROS in the liver. Aminochalcone 4AAF delays the clonic stage of the epileptic seizures . Aminochalcone 4AAF can be used in the study of anxiety, hyperglycemia, and seizures.
    Aminochalcone 4AAF
  • HY-151951
    Antidepressant agent 4
    Antidepressant agent 4 is an orally active antidepressant agent. Antidepressant agent 4 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 4
Cat. No. Product Name / Synonyms Application Reactivity