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-A0198S
    Adinazolam-d5
    		Agonist
    Adinazolam-d5 (U 41123-d5) is a deuterium labeled Adinazolam (HY-A0198). Adinazolam is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities.
    Adinazolam-d<sub>5</sub>
  • HY-183357
    GABAAR/5-HT2AR modulator-1
    		Agonist
    GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABAAR agonist and 5-HT2AR antagonist with Kd values of 0.89 and 0.78 μM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-α, IL-6, IL-1β, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-κB pathway activation by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage.
    GABAAR/5-HT2AR modulator-1
  • HY-179519
    Umbelopsisin A
    		Agonist
    Umbelopsisin A is a GABAA and GABAB non-selective agonist. Umbelopsisin A activates the GABAergic pathway, including notch signaling and fatty acid metabolism. Umbelopsisin A shows dual neuroprotection against glutamate excitotoxicity in vitro (reducing ROS and cell death) and in vivo. Umbelopsisin A can be used for the study of glaucoma and broader neurodegenerative disease applications.
    Umbelopsisin A
  • HY-100140A
    Pipequaline hydrochloride
    		Agonist 99.69%
    Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline hydrochloride
  • HY-125508
    CCD-3693
    		Agonist
    CCD-3693 is an orally active GABA receptor agonist. CCD-3693 has anxiolytic, anticonvulsant and sedative hypnotic activities and can be used in research related to neurological diseases.
    CCD-3693
  • HY-103535
    GBLD345
    		Agonist
    GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM).
    GBLD345
  • HY-B1715R
    Oxiracetam (Standard)
    		Agonist
    Oxiracetam (Standard) is the analytical standard of Oxiracetam. This product is intended for research and analytical applications. Oxiracetam (ISF2522) is an orally active and a BBB-penetrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases.
    Oxiracetam (Standard)
  • HY-100140R
    Pipequaline (Standard)
    		Agonist
    Pipequaline (Standard) is the analytical standard of Pipequaline. This product is intended for research and analytical applications. Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline (Standard)
  • HY-17030R
    Acamprosate calcium (Standard)
    		Agonist
    Acamprosate (calcium) (Standard) is the analytical standard of Acamprosate (calcium). This product is intended for research and analytical applications.
    Acamprosate calcium (Standard)
  • HY-A0173R
    Progabide (Standard)
    		Agonist
    Progabide (Standard) is the analytical standard of Progabide. This product is intended for research and analytical applications. Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.
    Progabide (Standard)
  • HY-119687R
    Bifenazate (Standard)
    		Agonist
    Bifenazate (Standard) is the analytical standard of Bifenazate. This product is intended for research and analytical applications. Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor. Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III.
    Bifenazate (Standard)
  • HY-101869R
    MK-0343 (Standard)
    		Agonist
    MK-0343 (Standard) is the analytical standard of MK-0343. This product is intended for research and analytical applications. MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.
    MK-0343 (Standard)
  • HY-101639AR
    CP-409092 hydrochloride (Standard)
    		Agonist
    CP-409092 (hydrochloride) (Standard) is the analytical standard of CP-409092 (hydrochloride) (HY-101639A). This product is intended for research and analytical applications. CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity.
    CP-409092 hydrochloride (Standard)
  • HY-105056R
    Bretazenil (Standard)
    		Agonist
    Bretazenil (Standard) is the analytical standard of Bretazenil (HY-105056). This product is intended for research and analytical applications. Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects.
    Bretazenil (Standard)
  • HY-100810R
    Isoguvacine hydrochloride (Standard)
    		Agonist
    Isoguvacine (hydrochloride) (Standard) is the analytical standard of Isoguvacine (hydrochloride) (HY-100810). This product is intended for research and analytical applications. Isoguvacine hydrochloride is a GABA receptor agonist.
    Isoguvacine hydrochloride (Standard)
  • HY-136942
    DS1
    		Agonist
    DS1 is a potent GABAA agonist. DS1 increases the activity of serum response element (SRE) and cAMP response element (CRE) promoters. DS1 induces luteinizing hormone beta (LHbeta) and follicle-stimulating hormone beta (FSHbeta) promoter activity.
    DS1
  • HY-129710
    CGP47656
    		Agonist
    CGP47656 is a potent GABAB receptor agonist that inhibits Forskolin (HY-15371)-stimulated adenylyl cyclase activity and augments noradrenaline-stimulated adenylyl cyclase activity. CGP47656 is promising for research of brain function-related diseases.
    CGP47656
  • HY-101059R
    FGIN 1-27 (Standard)
    		Agonist
    FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27. This product is intended for research and analytical applications. FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions.
    FGIN 1-27 (Standard)
  • HY-W765182
    Emamectin-d3
    		Agonist
    Emamectin-d3 is the deuterium labeled Emamectin. Emamectin is a macrocyclic lactone insecticide. Emamectin acts as agonist for GABA-gated chloride channels.
    Emamectin-d<sub>3</sub>
  • HY-14856
    Atagabalin
    		Agonist
    Atagabalin (PD 0200390) is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety and sedative effects. Atagabalin enhances the activity of the GABA receptor by binding to the α2δ subunit of the GABA receptor, thereby increasing the GABA mediated inhibition. This enhancement results in reduced excitability of neurons, helping to reduce anxiety and improve sleep. Atagabalin can be used to study neuropsychiatric disorders, anxiety or sleep disorders.
    Atagabalin
Cat. No. Product Name / Synonyms Application Reactivity