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-168758
    Delta3,5-cholestadien-7-one
    		Modulator
    Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.
    Delta3,5-cholestadien-7-one
  • HY-B1606
    Chlorothymol
    		Activator 99.49%
    Chlorothymol (Chlorthymol) is a potent GABAA receptor subunit LGC-37 positive modulator. Chlorothymol is an effective anticonvulsant. Chlorothymol is protective in several mouse seizure assays, including the 6-Hz 44-mA model of pharmacoresistant seizures. Chlorothymol possess GABAergic, membrane-modifying, antioxidant and topical antiseptic properties.
    Chlorothymol
  • HY-B0007B
    (S)-Baclofen
    		Agonist
    (S)-Baclofen is a selective GABAB receptor agonist with the IC50 values of 1.77 μM and 1564 μM for GABAB and GABAA, respectively.
    (S)-Baclofen
  • HY-N8472
    Chrodrimanin B
    		Antagonist
    Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on?B.?mori GABAR RDL with an IC50?of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC50?of 1.66 nM.?Chrodrimanin B, a meroterpenoid, shows insecticidal activity.
    Chrodrimanin B
  • HY-B0009R
    Flumazenil (Standard)
    		Antagonist
    Flumazenil (Standard) is the analytical standard of Flumazenil. This product is intended for research and analytical applications. Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
    Flumazenil (Standard)
  • HY-103530R
    CGP35348 (Standard)
    		Antagonist
    CGP35348 (Standard) is the analytical standard of CGP35348. This product is intended for research and analytical applications. CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only[1]. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage[2].
    CGP35348 (Standard)
  • HY-100813R
    Saclofen (Standard)
    		Antagonist
    Saclofen (Standard) is the analytical standard of Saclofen.
    Saclofen (Standard)
  • HY-W103463
    1-Phenyl-2-pyrrolidinone
    		Inhibitor 99.86%
    1-Phenyl-2-pyrrolidinone (1-Phenylpyrrolidin-2-one) is a phenyl analogue of GABA with sedative effect, decreasing the exploratory behavior of rats at 50-100 mg/kg (i.v.). 1-Phenyl-2-pyrrolidinone also has been proved to inhibit emotional reactions in dogs and cats. 1-Phenyl-2-pyrrolidinone induces decreases in the pressor reaction to emotional stress without accompanied by normalization of the function of baroreceptor reflexes.
    1-Phenyl-2-pyrrolidinone
  • HY-117106
    PNU-107484A
    PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl- currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes.
    PNU-107484A
  • HY-16579AR
    Etifoxine (Standard)
    		Activator
    Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
    Etifoxine (Standard)
  • HY-101596
    Ethyl dirazepate
    Ethyl dirazepate is a agent which is a benzodiazepine derivative. It has anxiolytic and possibly other characteristic benzodiazepine properties.
    Ethyl dirazepate
  • HY-19065
    Ru-32514
    		Agonist
    Ru-32514 is an agonist of benzodiazepine receptor.
    Ru-32514
  • HY-19250
    U-101017
    		Agonist
    U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects. 
    U-101017
  • HY-B0340R
    Nefiracetam (Standard)
    		Activator
    Nefiracetam (Standard) is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.
    Nefiracetam (Standard)
  • HY-B0122S
    Topiramate-13C6
    		Activator
    Topiramate-13C6 (McN 4853-13C6) is the 13C labeled isotope of Topiramate (HY-B0122). Topiramate (McN 4853) 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-<sup>13</sup>C<sub>6</sub>
  • HY-W025443
    6-(4-Methoxyphenyl)pyridazin-3-amine
    		Antagonist
    6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive GABA-A receptor antagonist.
    6-(4-Methoxyphenyl)pyridazin-3-amine
  • HY-10232S
    THIP-d4
    		Antagonist
    THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
    THIP-d<sub>4</sub>
  • HY-155381
    APS3
    		Inhibitor
    APS3 is a GABA and nACh receptors inhibitor, with a LC50 of 7.2423 μg/mL against Plutella xylostella.
    APS3
  • HY-124225
    RU 33965
    		Agonist
    RU 33965 is an orally active benzodiazepine receptor weak partial inverse agonist.
    RU 33965
  • HY-B1833R
    Afloqualone (Standard)
    		Agonist
    Afloqualone (Standard) is the analytical standard of Afloqualone. This product is intended for research and analytical applications. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome.
    Afloqualone (Standard)
Cat. No. Product Name / Synonyms Application Reactivity