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-103534
    CI-966 hydrochloride
    		Inhibitor 99.60%
    CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.
    CI-966 hydrochloride
  • HY-N9483
    7-Keto-DHEA
    		Modulator 98.89%
    7-Keto-DHEA binds to GABA Receptor, and reduces the ethanol intake in rats. 7-Keto-DHEA exhibits potential in investigation of alcohol dependence disorders.
    7-Keto-DHEA
  • HY-124285
    ATPCA hydrochloride
    ATPCA hydrochloride is a selective radioactive substrate for BGT1 over GAT1/GAT3.
    ATPCA hydrochloride
  • HY-108295
    Pivagabine
    		Antagonist 98.0%
    Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
    Pivagabine
  • HY-B0649S1
    Propofol-d18
    		Activator
    Propofol-d18 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission.
    Propofol-d<sub>18</sub>
  • HY-P2602
    α-Casozepine
    		99.36%
    α-Casozepine is a bioactive peptide derived from the α protein S1 casein in milk and has an affinity for γ-aminobutyric acid (GABA) receptors in the brain. α-Casozepine has anti-anxiety effects.
    α-Casozepine
  • HY-116813
    ZK 93423
    		Agonist 99.43%
    ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents.
    ZK 93423
  • HY-125296
    Fipronil sulfone
    		Inhibitor 99.75%
    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
  • HY-18715
    Ornidazole (Levo-)
    		98.86%
    Levo-ornidazole ((S)-Ornidazole) is the L-isomer of Ornidazole. Ornidazole (Levo-) increases GAD 65/67 expression and decreases brain Glu/GABA ratio. Ornidazole (Levo-) has a mild sedative effect. Levo-ornidazole can be used in the research of anti-anaerobic and anti-parasitic agents.
    Ornidazole (Levo-)
  • HY-101359
    TPMPA
    		Antagonist 98.1%
    TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells.
    TPMPA
  • HY-105272
    Loreclezole
    		Agonist 99.97%
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
    Loreclezole
  • HY-115685
    3-Methyl-GABA
    		Activator 99.86%
    3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABAA receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity.
    3-Methyl-GABA
  • HY-B0211R
    Riluzole (Standard)
    		Inhibitor
    Riluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. 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.
    Riluzole (Standard)
  • HY-120837
    PZ-II-029
    		Agonist 99.23%
    PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects.
    PZ-II-029
  • HY-W067716
    Spinacine
    		Inhibitor
    Spinacine is an alkaloid inhibitor of GABA (γ-aminobutyric acid) absorption that can be isolated from spinach leaf extract.
    Spinacine
  • 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-137494
    Ethyl β-carboline-3-carboxylate
    		99.75%
    Ethyl β-carboline-3-carboxylate (fl-CCE) is a ligand and short-acting antagonist of benzodiazepine receptors. Ethyl β-carboline-3-carboxylate did not affect cerebellar cGMP levels when used alone, but when taken together with Diazepam, it significantly inhibited the cGMP levels that were upregulated by Diazepam.
    Ethyl β-carboline-3-carboxylate
  • HY-108403
    Phenibut
    		Agonist 99.88%
    Phenibut (β-Phenyl-GABA) is a GABA-B agonist. Phenibut acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut has anxiolytic and nootropic (cognition enhancing) effects.
    Phenibut
  • HY-116622
    α5IA
    		Agonist
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential.
    α5IA
  • HY-W008645
    NCS-382 sodium
    		Antagonist 99.0%
    NCS-382 (sodium) is a potent GABA receptor antagonist. NCS-382 (sodium) has anti-sedative and anti-hypnotic activities and can be used in research related to neurological diseases.
    NCS-382 sodium
Cat. No. Product Name / Synonyms Application Reactivity