2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. GABA Receptor

GABA Receptor

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.

GABA Receptor Related Products (596):

Cat. No. Product Name Effect Purity
  • HY-B0211
    Riluzole Inhibitor 99.80%
    Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-107994
    Aminooxyacetic acid hemihydrochloride Inhibitor
    Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
  • HY-N0219
    Bicuculline Antagonist
    Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice[1][2][3][4].
  • HY-B0649
    Propofol Activator 99.52%
    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[1].
  • HY-N0067
    γ-Aminobutyric acid Agonist
    γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system[1][2].
  • HY-173251S
    ENX-101 Modulator
    ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models[1].
  • HY-172588
    GABAA receptor modulator-7 Modulator
    GABAA receptor modulator-7 (compound 1m), a spiro-Barbiturate, is a GABAA receptor modulator. GABAA receptor modulator-7 reverses the action of anesthetics without affecting GABA-induced desensitization and can be used for study of antiepileptics and anxiolytics[1].
  • HY-173413
    Insecticidal agent 21
    Insecticidal agent 21 (Compound 6) is an insecticide that is effective against Culex pipiens larvae (LC50: 0.4 μg/mL). Insecticidal agent 21 achieves multi-target neurotoxicity by inhibiting acetylcholinesterase (AChE) and simultaneously targeting other neural receptors (nicotinic acetylcholine receptors (nAChR), voltage-gated sodium channels (VGSC), and γ-aminobutyric acid receptors (GABAAR)). Insecticidal agent 21 has a strong insecticidal effect and can be used in the development of new insecticides to address the problem of mosquito resistance to traditional insecticides[1].
  • HY-103501
    SB-205384 Modulator
    SB-205384 is a GABAA receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist[1].
  • HY-131941
    SJM-3 Agonist
    SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface[1].
  • HY-103510
    TB-21007 Agonist 99.7%
    TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats[1].
  • HY-119687
    Bifenazate Agonist 99.89%
    Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm[1]. Bifenazate is a positive allosteric modulator of GABA receptor[2]. Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III[3].
  • HY-103533R
    Gabazine (Standard) Antagonist
    Gabazine (Standard) is the analytical standard of Gabazine. This product is intended for research and analytical applications. Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
  • 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[1].
  • HY-14840
    Phenylpiracetam Activator 99.91%
    Phenylpiracetam(Phenotropyl; Phenotropil) is a phenylated derivative of the nootropic drug piracetam.
  • HY-12783
    SCH 50911 hydrochloride Antagonist
    SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
  • HY-101411S
    4-Acetamidobutanoic acid-d3 Agonist
    4-Acetamidobutanoic acid-d3 is the deuterated analog of 4-Acetamidobutanoic acid (HY-101411). 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities[1].
  • HY-118301
    ADX71441 Modulator
    ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity[1].
  • HY-P5188A
    Waglerin-1 Inhibitor 98.71%
    Waglerin-1, a 22-amino acid peptide, is a competitive antagonist of the muscle nicotinic receptor (nAChR)[1].
  • 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[1][2].