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-118207
    LU-32-176B
    		Inhibitor
    LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively.
    LU-32-176B
  • HY-116859
    Ro 14-7437
    		Antagonist
    Ro 14-7437 is a potent and selective potentiating antagonist of Midazolam.
    Ro 14-7437
  • HY-116457
    Propanidid
    		Agonist
    Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA) receptor agonist and a short-acting non-barbiturate general agent that can suppress or relieve pain. Propanidid can decrease the arterial pressure.
    Propanidid
  • HY-117256
    Gabazine free base
    		Antagonist
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of 0.2 μM for GABA receptor.
    Gabazine free base
  • HY-10061A
    Lesogaberan napadisylate
    		Agonist
    Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan napadisylate
  • HY-159826
    Brexanolone caprilcerbate
    		Agonist
    Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator.
    Brexanolone caprilcerbate
  • HY-146280
    mGAT3/4-IN-1
    		Inhibitor
    mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice.
    mGAT3/4-IN-1
  • HY-169432
    TET-13
    		Modulator
    TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively).
    TET-13
  • HY-13694R
    Methionine (Standard)
    		Activator
    Methionine (Standard) is the analytical standard of Methionine. This product is intended for research and analytical applications. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine (Standard)
  • HY-107782R
    Picrotin (Standard)
    Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0355R
    Ginkgolide A (Standard)
    		Antagonist
    Ginkgolide A (Standard) is the analytical standard of Ginkgolide A. This product is intended for research and analytical applications. Ginkgolide A (BN-52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist.
    Ginkgolide A (Standard)
  • HY-139145
    Etbicyphat
    		Antagonist ≥98.0%
    Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors.
    Etbicyphat
  • HY-119605
    DAA-1097
    		Agonist
    DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects.
    DAA-1097
  • HY-N0662R
    Amentoflavone (Standard)
    		Modulator
    Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.
    Amentoflavone (Standard)
  • HY-106851
    Panadiplon
    		Agonist
    Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.
    Panadiplon
  • HY-P5860
    MmTx1 toxin
    		Modulator
    MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor susceptibility to agonist.
    MmTx1 toxin
  • HY-103518
    CGP36216
    		Antagonist
    CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders.
    CGP36216
  • HY-119105
    LY81067
    LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites.
    LY81067
  • HY-103513
    GABAA receptor agent 2
    		Modulator
    GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
    GABAA receptor agent 2
  • HY-19438
    Divaplon
    		Agonist
    Divaplon is a GABA receptor agonist with the EC50 values of 31 and 2 nM for α3β2γ2 and α5β2γ2, respectively. Divaplon shows anxiolytic activity.
    Divaplon
Cat. No. Product Name / Synonyms Application Reactivity