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

Related Products

PDF 3.03 MB

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-163855
    KGP-25
    KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for general anesthesia.
    KGP-25
  • HY-14953
    Imepitoin
    		Agonist 99.87%
    Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
    Imepitoin
  • HY-179215
    OV329 hydrochloride
    		Inhibitor 99.83%
    OV329 hydrochloride is a potent GABA aminotransferase inactivator. OV329 hydrochloride is a Vigabatrin (HY-15399) analogue. OV329 hydrochloride can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 hydrochloride exhibits anticonvulsant and antiepileptic activities. OV329 hydrochloride can be used for the research of neurological disease, such as seizure.
    OV329 hydrochloride
  • HY-154436
    Anticonvulsant agent 2
    		Inhibitor
    Anticonvulsant agent 2 is a potent and orally active anticonvulsant agent. Anticonvulsant agent 2 shows antiepileptic activity.
    Anticonvulsant agent 2
  • HY-109009A
    (S)-Padsevonil
    		Modulator 99.40%
    (S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
    (S)-Padsevonil
  • HY-B2090
    Pipazethate
    		Antagonist 99.0%
    Pipazethate (SKF 70230A), a pyridobenzothiazine derivative, is a potent GABA antagonist. Pipazethate has antitussive activity. Pipazethate can be used in research in cough supressant.
    Pipazethate
  • HY-124534
    (1S,3R)-3-Aminocyclopentane carboxylic acid
    		≥98.0%
    (1S,3R)-3-Aminocyclopentane carboxylic acid has GABAA receptor activity.
    (1S,3R)-3-Aminocyclopentane carboxylic acid
  • HY-123840
    MRK-623
    		Agonist 98.73%
    MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect.
    MRK-623
  • HY-16974R
    Afoxolaner (Standard)
    		Inhibitor
    Afoxolaner (Standard) is the analytical standard of Afoxolaner. This product is intended for research and analytical applications. Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
    Afoxolaner (Standard)
  • HY-Y0313R
    p-Hydroxybenzaldehyde (Standard)
    		Antagonist
    p-Hydroxybenzaldehyde (Standard) is the analytical standard of p-Hydroxybenzaldehyde. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0692R
    Cefepime (Standard)
    		Inhibitor
    Cefepime (BMY-28142) (Standard) is the analytical standard of Cefepime. This product is intended for research and analytical applications. Cefepime is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
    Cefepime (Standard)
  • HY-133594
    Sandaracopimaric acid
    		Inhibitor 98.86%
    Sandaracopimaric acid is a diterpenoid with anti-inflammatory effect. Sandaracopimaric acid reduces the contraction of phenylephrine-induced pulmonary arteries with an EC50 of 43.93 μM.
    Sandaracopimaric acid
  • HY-113320S
    Etiocholanolone-d5
    		Modulator 99.20%
    Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form.
    Etiocholanolone-d<sub>5</sub>
  • HY-100140
    Pipequaline
    		Agonist 99.93%
    Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline
  • 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-Y1176R
    Isonipecotic acid (Standard)
    		Agonist
    Isonipecotic acid is a GABAA receptor partial agonist.
    Isonipecotic acid (Standard)
  • HY-101639
    CP-409092
    		Agonist
    CP-409092 is a partial agonist of GABAA receptor, with anti-anxiety activity.
    CP-409092
  • HY-B0122S
    Topiramate-13C6
    		Activator 99.67%
    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-122489A
    (S)-Laudanosine
    		Control 99.95%
    (S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM).
    (S)-Laudanosine
Cat. No. Product Name / Synonyms Application Reactivity