GABA Receptors

Gamma-aminobutyric acid (GABA) receptor agonists, antagonists and modulators target inhibitory neurotransmission. GABA-A receptors are ligand-gated chloride channels, and their cloning in 1987 placed them among the other ligand-gated ion channel receptors. GABA-B receptors are G protein-coupled receptors, and their cloning in 1997 revealed similarity to metabotropic glutamate receptors. Flumazenil blocks the benzodiazepine site of GABA-A receptors, whereas the anesthetic propofol enhances GABA-A receptor currents. Natural products such as baicalin and dihydromyricetin are also listed for their reported activity at GABA-A receptors. These ligands support studies of synaptic inhibition, neuronal excitability, sedation and anxiety-related behavior.

11 Items

  • 6'''-Feruloylspinosin
    Cat. No.
    A15732

    6'''-Feruloylspinosin

    6'''-Feruloylspinosin is a flavonoid that acts as a GABA receptor activator. Isolated from the seeds of Ziziphus jujuba, it is capable of crossing the blood-brain barrier and enhancing the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons. This compound is valuable for research focused on neurological disorders and the modulation of GABAergic signaling pathways.

    1 mg
    $30.00
    5 mg
    $70.00
    All 4 sizes
  • 2'-O-Methylisoliquiritigenin
    Cat. No.
    A46040

    2'-O-Methylisoliquiritigenin

    2'-O-Methylisoliquiritigenin is a GABA receptor activator that enhances neurotransmitter activity across various pathways, including serotonin (5-HT), norepinephrine (NE), dopamine (DA), and GABA. Isolated from the Arachis species, this compound plays a significant role in modulating nervous system functions and offers valuable insights for research applications related to neurochemistry and pharmacology. Its selective influence on neurotransmitter pathways makes it a useful tool for studying neuropharmacological mechanisms.

    1 mg
    $95.00
    5 mg
    $235.00
    All 4 sizes
  • alpha-Asarone
    Cat. No.
    A66601

    alpha-Asarone

    Synonyms: α-Asarone; trans-Asarone

    Alpha-Asarone (α-Asarone) acts as a GABA receptor activator, demonstrating significant antidepressant-like activity in preclinical mouse models. This compound is of interest in neuropharmacology research for its potential effects on mood regulation and anxiety disorders. Its mechanism may provide insights into novel therapeutic approaches for treating depression and related conditions.

    200 mg
    $25.00
    500 mg
    $30.00
    All 3 sizes
  • Kavain
    Cat. No.
    A66618

    Kavain

    Kavain is a kavalactone derived from Piper methysticum, primarily acting as a GABA receptor activator. This compound has demonstrated anxiolytic effects in both animal and human studies. Its ability to positively modulate the gamma-aminobutyric acid type A (GABAA) receptor makes it relevant for research into anxiety disorders and related neurological conditions.

    10 mg
    $25.00
    50 mg
    $45.00
    All 4 sizes
  • Homocarnosine TFA
    Cat. No.
    A66629

    Homocarnosine TFA

    Synonyms: L-Homocarnosine TFA

    Homocarnosine TFA is a dipeptide comprised of γ-aminobutyric acid (GABA) and histidine, primarily found in the brain. As a GABA receptor activator, it functions as an inhibitory neuromodulator, demonstrating anticonvulsant properties. Additionally, Homocarnosine TFA exhibits antioxidant and anti-inflammatory activities, aids in the prevention of DNA damage, and inhibits the formation of advanced glycation end-products, making it relevant for various neurological research applications.

    5 mg
    $150.00
    10 mg
    $235.00
    All 3 sizes
  • 6-Methylflavone
    Cat. No.
    A66644

    6-Methylflavone

    6-Methylflavone is an activator of GABAA receptors, specifically targeting the α1β2γ2L and α1β2 subtypes. This compound demonstrates anxiolytic and sedative properties, making it of interest in neuropharmacological research. Its applications include studies on neuronal signaling and the modulation of inhibitory neurotransmission, contributing to the understanding of GABAergic system functions.

    100 mg
    $20.00
    200 mg
    $25.00
    All 2 sizes
  • Cirsimaritin
    Cat. No.
    A66658

    Cirsimaritin

    Cirsimaritin is a GABA receptor activator that exhibits weak binding to the benzodiazepine site on GABAA receptors. It demonstrates notable antidepressant, anxiolytic, and antinociceptive activities, making it a valuable tool for research in neuropharmacology. Its potential applications include the exploration of anxiety disorders, depression, and pain management pathways.

    1 mg
    $40.00
    5 mg
    $100.00
    All 5 sizes
  • 3-Methyl-GABA
    Cat. No.
    A66670

    3-Methyl-GABA

    3-Methyl-GABA is a potent GABA aminotransferase activator that enhances the activity of L-glutamic acid decarboxylase (GAD). This compound fits into the binding pocket of the GABAA receptor (GABAaR), facilitating the modulation of GABAergic signaling. 3-Methyl-GABA demonstrates anticonvulsant properties, making it a valuable reagent for research in neuropharmacology and the study of seizure disorders.

    5 mg
    $150.00
    10 mg
    $250.00
    All 5 sizes
  • N-Arachidonyl-GABA
    Cat. No.
    A66695

    N-Arachidonyl-GABA

    N-Arachidonyl-GABA is a novel lipoamino acid that acts as a GABA receptor activator. It has been identified in bovine brain and exhibits significant analgesic activity. This compound is valuable for research on pain modulation and GABAergic signaling pathways in various physiological contexts.

    Out of stock

    All 3 sizes
  • RuBi-GABA
    Cat. No.
    A66714

    RuBi-GABA

    RuBi-GABA is a ruthenium-based caged GABA compound that targets GABA receptors. Upon excitation with visible light wavelengths, RuBi-GABA undergoes photocleavage, effectively releasing GABA. This compound facilitates GABA receptor-mediated currents, making it an invaluable tool for research applications in neuropharmacology and photophysiology to study synaptic transmission and neuronal activity.

    10 mg
    $585.00
    All 1 sizes
  • Emamectin B1a
    Cat. No.
    A66919

    Emamectin B1a

    Synonyms: L-656,748

    Emamectin B1a is a semisynthetic derivative of avermectin B1a that serves as a GABA receptor activator. It enhances GABA responses by binding to GABAA receptors, demonstrating IC50 values of 57 nM for α1β1γ2, 210 nM for α1β2γ2, and 49.8 nM for α1β3γ2. Additionally, Emamectin B1a interacts with glycine receptors, exhibiting an IC50 of 218 nM in rat spinal cord. Its potent activity is evident in pest control applications, achieving 90% mortality in S. exigua larvae at concentrations as low as 1.067 ng/mL in foliar spray bioassays and topical applications.

    1 mg
    $600.00
    All 1 sizes

11 Items

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