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-103509
    NNC 05-2090 hydrochloride
    		Inhibitor 99.09%
    NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.
    NNC 05-2090 hydrochloride
  • HY-N2368
    Arecaidine
    		Inhibitor 99.58%
    Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine
  • HY-100800
    TACA
    		Agonist 99.33%
    TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.
    TACA
  • HY-114883A
    Homocarnosine TFA
    		99.67%
    Homocarnosine TFA is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine TFA is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects. Homocarnosine TFA has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.
    Homocarnosine TFA
  • HY-N6084
    Humulone
    		Activator 99.46%
    Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
    Humulone
  • HY-100370
    MRK-016
    		Antagonist 99.71%
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA?α1β3γ2, GABAA?α2β3γ2, GABAA?α3β3γ2, and GABAA?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
    MRK-016
  • HY-69359
    Nipecotic acid
    		Inhibitor ≥98.0%
    Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300?μM.
    Nipecotic acid
  • HY-103519
    rac-BHFF
    		Activator 98.18%
    rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor.
    rac-BHFF
  • HY-N6648
    Cirsimaritin
    		99.23%
    Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin
  • HY-107782
    Picrotin
    		99.92%
    Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission.
    Picrotin
  • HY-19371
    Lorediplon
    		Modulator 99.88%
    Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
    Lorediplon
  • HY-N6630
    6-Methylflavone
    		Activator 99.77%
    6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
    6-Methylflavone
  • HY-B0340
    Nefiracetam
    		Activator 99.91%
    Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal systems enhancer for Ro 5-4864-induced convulsions.
    Nefiracetam
  • HY-121599
    CGP 36742
    		Antagonist ≥98.0%
    CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression.
    CGP 36742
  • HY-N2080
    Songorine
    		Antagonist 99.69%
    Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
    Songorine
  • HY-121618
    α-Thujone
    		Modulator 98.07%
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
    α-Thujone
  • HY-Y1683
    DL-Menthol
    		Activator ≥98.0%
    DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor.
    DL-Menthol
  • HY-107489
    RO 4938581
    		Antagonist 99.30%
    RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
    RO 4938581
  • HY-N0301
    Thiocolchicoside
    		Antagonist 99.54%
    Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
    Thiocolchicoside
  • HY-101869
    MK-0343
    		Agonist 99.31%
    MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.
    MK-0343
Cat. No. Product Name / Synonyms Application Reactivity