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-125296R
    Fipronil sulfone (Standard)
    		Inhibitor
    Fipronil sulfone (Standard) is the analytical standard of Fipronil sulfone. This product is intended for research and analytical applications. Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
    Fipronil sulfone (Standard)
  • HY-B1122R
    L-Cycloserine (Standard)
    		Inhibitor
    L-Cycloserine (Standard) is the analytical standard of L-Cycloserine. This product is intended for research and analytical applications. L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacterium tuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains[1][2][3][4].
    L-Cycloserine (Standard)
  • HY-N2096R
    Kavain (Standard)
    		Activator
    Kavain (Standard) is the analytical standard of Kavain. This product is intended for research and analytical applications. Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
    Kavain (Standard)
  • HY-172433
    Refisolone
    		Antagonist
    Refisolone is an antagonist of the GABAA receptor.
    Refisolone
  • HY-117955
    GMA-839
    		Modulator
    GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics.
    GMA-839
  • HY-135482
    GABAA receptor agent 2 TFA
    		Antagonist
    GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).
    GABAA receptor agent 2 TFA
  • HY-174152
    GABAB receptor antagonist 5
    		Antagonist
    GABAB receptor antagonist 5 (Compound 23) is a competitive GABAB receptor antagonist. GABAB receptor antagonist 5 is promising for research of neuropsychiatric diseases, such as epilepsy, depression, and addiction.
    GABAB receptor antagonist 5
  • HY-17001AR
    Flupirtine (Standard)
    		Activator
    Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
    Flupirtine (Standard)
  • HY-113413R
    Imidazoleacetic acid (Standard)
    		Agonist
    Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity.
    Imidazoleacetic acid (Standard)
  • HY-170902
    GABAA receptor modulator-4
    		Modulator
    GABAA receptor modulator-4 (Compound 4) is the negative allosteric modulator for GABAA receptor. GABAA receptor modulator-4 inhibits α1β3γ2 GABAA receptor-mediated peak and steady currents with IC50 of 10 μM and 10 μM.
    GABAA receptor modulator-4
  • HY-182944
    GATT-44
    		Ligand
    GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC50 of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated 18F-radiofluorination. The radiolabeled GATT-44 ([18F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases.
    GATT-44
  • HY-B0649R
    Propofol (Standard)
    		Activator
    Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
    Propofol (Standard)
  • HY-W028389
    Pyrazolam
    Pyrazolam is a brominated triazolo benzodiazepine psychoactive substance with oral effectiveness. Pyrazolam produces anxiolytic, sedative, and sleep-promoting effects. Pyrazolam can be used for the research of anxiety.
    Pyrazolam
  • HY-Y0313S2
    p-Hydroxybenzaldehyde-d5
    p-Hydroxybenzaldehyde-d5 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde-d<sub>5</sub>
  • HY-111194
    Ro 22-8515
    		Ligand
    Ro 22-8515 is a ligand of Benzodiazepine receptor.
    Ro 22-8515
  • HY-W742312
    Brallobarbitone
    		Modulator
    Brallobarbitone is a positive allosteric modulator of GABAA receptor. Brallobarbitone can be used in the research of β-cell dysfunction.
    Brallobarbitone
  • HY-129431
    U-89843A
    		Activator 99.26%
    U-89843A (PNU-89843) is a GABAA receptors positive allosteric modulator (PAM). U-89843A enhances GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A shows antioxidant and sedative effects.
    U-89843A
  • HY-105059
    Denzimol
    		Inhibitor
    Denzimol is an orally active anticonvulsant agent.
    Denzimol
  • HY-135034
    UMB68 sodium
    UMB68 sodium is a selective GHB receptor ligand. UMB68 sodium displaces [3H]NCS-382 with an IC50 of 38 nM in rat cerebrocortical membranes. UMB68 sodium has no significant affinity at GABAB receptors, cannot be metabolized to GABA-active compounds.
    UMB68 sodium
  • HY-147736
    GABAA receptor agonist 2
    		Agonist
    GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression.
    GABAA receptor agonist 2
Cat. No. Product Name / Synonyms Application Reactivity