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-147657
    GABAA receptor modulator-2
    		Modulator
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety.
    GABAA receptor modulator-2
  • HY-155498
    TETS-4-Methylaniline
    		Inhibitor
    TETS-4-Methylaniline (compound 2k) is a hapten. TETS-4-Methylaniline conjugates to the carrier protein via using either diazotization or glutaraldehyde methods.
    TETS-4-Methylaniline
  • HY-103526
    DPNI-GABA
    		Inhibitor
    DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC50 value of 0.5 mM.
    DPNI-GABA
  • HY-173616
    GABAA receptor modulator-8
    		Agonist
    GABAA receptor modulator-8 (10c) is a blood-brain barrier penetrated, selective and positive modulator of GABAA receptor, with excellent antiepileptic activity.
    GABAA receptor modulator-8
  • HY-P11208A
    mNLS-CPP-scramble
    		Control
    mNLS-CPP-scramble is a negative control peptide of mNLS-CPP-WSTF. mNLS-CPP-scramble is promising for research of chronic inflammatory diseases (e.g., MASH, osteoarthritis).
    mNLS-CPP-scramble
  • HY-168986
    Moxetomidate
    		Agonist
    Moxetomidate is a GABAA receptor agonist with hypnotic effect.
    Moxetomidate
  • HY-B1594R
    Carbromal (Standard)
    		Agonist
    Carbromal (Standard) is the analytical standard of Carbromal. This product is intended for research and analytical applications. Carbromal (Adalin; Adisomnol) is a sedative with centrally depressant effects.
    Carbromal (Standard)
  • HY-103495
    17-PA
    		Antagonist
    17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABAA receptors.
    17-PA
  • HY-W007686R
    Imidazoleacetic acid hydrochloride (Standard)
    Imidazoleacetic acid (hydrochloride) (Standard) is the analytical standard of Imidazoleacetic acid (hydrochloride). This product is intended for research and analytical applications. Imidazoleacetic acid hydrochloride is a γ-aminobutyric acid receptor agonist. Imidazoleacetic acid hydrochloride inhibits GABA-T in a non-competitive manner, with a Ki value of 0.34 mM. Imidazoleacetic acid hydrochloride increases total free GABA in brain[1][2][3].
    Imidazoleacetic acid hydrochloride (Standard)
  • HY-110234R
    Topiramate D12 (Standard)
    		Activator
    Topiramate D12 (Standard) is the analytical standard of Topiramate D12. This product is intended for research and analytical applications. Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
    Topiramate D12 (Standard)
  • HY-106547
    Rilmazafone
    Rilmazafone is a benzodiazepine (omega) ligand and an orally active sleep inducer.
    Rilmazafone
  • HY-169193
    Azocarnil
    		Agonist
    Azocarnil is a GABAergic agonist-potentiator. Azocarnil can be used in neurological research.
    Azocarnil
  • HY-123249
    HZ166
    		Agonist
    HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects. HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HZ166
  • HY-Y0313S1
    p-Hydroxybenzaldehyde-13C
    		Antagonist
    p-Hydroxybenzaldehyde-13C is the 13C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde-<sup>13</sup>C
  • HY-U00199A
    (S)-Norzopiclone
    		Agonist
    (S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABAA receptor and inhibits nACh and NMDA receptors.
    (S)-Norzopiclone
  • HY-161896
    Transcription factor-IN-1
    		Inhibitor
    Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED50 =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models.
    Transcription factor-IN-1
  • HY-14758
    Adipiplon
    		Agonist
    Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.
    Adipiplon
  • 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-P11208
    mNLS-CPP-WSTF
    		Inhibitor
    mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA.
    mNLS-CPP-WSTF
  • HY-130349
    Emamectin B1a
    		Activator
    Emamectin B1a (L-656,748) is a semisynthetic derivative of avermectin B1a that binds to GABA receptors (Ki=17.6 nM in rat brain membranes) and enhances GABA responses. Emamectin B1a acitivates GABAA receptors α1β1γ2, α1β2γ2, and α1β3γ2 with IC50s of 57, 210, and 49.8 nM, respectively. Emamectin B1a also binds to glycine receptors, inhibiting glycine receptors with an IC50=218 nM in rat spinal cord. Emamectin B1a (1.067 ng/mL) caused 90% mortality of S. exigua larvae in foliar spray bioassays and topical application, making it more toxic than avermectin B1.
    Emamectin B1a
Cat. No. Product Name / Synonyms Application Reactivity