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-114300
    DSP-0565
    		Agonist
    DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin.
    DSP-0565
  • HY-105627A
    Profadol hydrochloride
    		Agonist
    Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR.
    Profadol hydrochloride
  • HY-N0042R
    Ginsenoside Rc (Standard)
    		Agonist
    Ginsenoside Rc (Standard) is the analytical standard of Ginsenoside Rc. This product is intended for research and analytical applications. Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
    Ginsenoside Rc (Standard)
  • HY-100124
    Bamaluzole
    		Agonist
    Bamaluzole is a GABA receptor agonist extracted from patent WO 2012064642 A1.
    Bamaluzole
  • HY-B0007S2
    Baclofen-d5 hydrochloride
    		Agonist
    Baclofen-d5 hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
    Baclofen-d<sub>5</sub> hydrochloride
  • HY-D1704
    Bodipy TMR-X muscimol
    		Agonist 99.79%
    Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations.
    Bodipy TMR-X muscimol
  • HY-131997
    2'MeO6MF
    		Agonist
    2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
    2'MeO6MF
  • HY-118490
    T-2000
    		Agonist
    T-2000 (DMMDPB) is an orally active GABA receptor agonist with anticonvulsant activities.
    T-2000
  • HY-106635
    Suriclone
    		Agonist
    Suriclone (RP31264) is a GABA receptor agonist. Suriclone is an anxiolytic agent with a high affinity for the benzodiazepine receptors. Suriclone has oral activity.
    Suriclone
  • 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-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
  • HY-156061
    NAP-1
    		Agonist
    NAP-1 is a compound with agent that can suppress or relieve pain. effects. NAP-1 enhances the inhibitory current by binding to a specific site of GABAaR, resulting in a narcotic effect. NAP-1 can be used in research to develop clinical agent that can suppress or relieve pain.
    NAP-1
  • HY-167650
    Fletazepam
    		Agonist
    Fletazepam is a benzodiazepine derivative with sedative, anxiolytic and muscle relaxant effects. Fletazepam can be utilized in neurological research.
    Fletazepam
  • HY-160978
    Timelotem
    		Agonist
    Timelotem (KC-7507 free base) is a representative of a class of 1, 2-cyclo1, 4-benzodiazepines. Timelotem shows significant antipsychotic properties. Timelotem produces sedative, anti-anxiety and anti-convulsant effects by enhancing the action of the neurotransmitter gamma-aminobutyric acid (GABA). Timelotem can be used in studies of schizophrenia and other mental disorders.
    Timelotem
  • HY-B0007A
    (S)-Baclofen hydrochloride
    		Agonist
    (S)-Baclofen hydrochloride is a GABAB receptor agonist that crosses the blood-brain barrier and is orally active, with IC50 values ​​of 1.77 μM for GABAB and 1564 μM for GABAA. (S)-Baclofen hydrochloride can be used in research on muscle disorders such as spasticity.
    (S)-Baclofen hydrochloride
  • HY-116944
    Ro 17-1812
    		Agonist
    Ro 17-1812 is a benzodiazepine receptor partial agonist with anticonvulsant effect.
    Ro 17-1812
  • HY-100915
    SKF 97541
    		Agonist
    SKF 97541 (CGP 35024) is a potent and selective GABAB agonist that can induce hyperpotential. SKF 97541 has antiepileptic activity.
    SKF 97541
  • HY-103521
    Anxiolytic/nonsedative agent-1
    		Agonist
    Anxiolytic/nonsedative agent-1 (compound 2b) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.
    Anxiolytic/nonsedative agent-1
  • HY-116197
    CGP44532
    		Agonist
    CGP44532 is a GABAB receptor agonist with a pEC50 (geometric mean of the half-maximal effective concentration) value of 5.63 μM.
    CGP44532
  • HY-123478
    Fengabine
    		Agonist
    Fengabine is a GABAergic antidepressant agent. Fengabine can be used for the research of depression.
    Fengabine
Cat. No. Product Name / Synonyms Application Reactivity