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-101060
    FGIN 1-43
    		Inhibitor 98.96%
    FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN 1-43
  • HY-101060
    FGIN 1-43
    		Activator 98.96%
    FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN 1-43
  • 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-141672S1
    17β-Estradiol sulfate-d4 sodium
    		≥99.0%
    17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.
    17β-Estradiol sulfate-d<sub>4</sub> sodium
  • 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-W677042
    α-Androstenol
    		Modulator
    α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and human male axillary sweat. α-Androstenol is also a positive modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50=0.4 μM). α-Androstenol decreases immobility time in the forced swim test and increases time spent in the open arms of the elevated plus maze in mice. α-Androstenol protects against seizures induced by Pentylenetetrazole or electroshock with anxiolytic-like activity in mice.
    α-Androstenol
  • 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-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-100812
    2-Hydroxysaclofen
    		Antagonist ≥98.0%
    2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats.
    2-Hydroxysaclofen
  • HY-103512
    TP003
    		Agonist 98.99%
    TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors.
    TP003
  • HY-103507
    N-Arachidonyl-GABA
    		Activator ≥99.0%
    N-Arachidonoyl-GABA is one member of a new class of lipoamino acids related to anandamide identified in bovine brain. N-Arachidonoyl-GABA displays analgesic activity.
    N-Arachidonyl-GABA
  • HY-121116
    CGS 8216
    		Antagonist 99.85%
    CGS 8216, a benzodiazepine receptor antagonist, inhibits 3H-flunitrazepam (3H-FLU) binding to rat synaptosomal membranes in vitro at subnanomolar concentrations.
    CGS 8216
  • 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-107482
    Picamilon
    		Agonist 98.25%
    Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.
    Picamilon
  • 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-N8852
    6-Methoxyflavanone
    		Modulator 98.95%
    6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABAA receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABAA receptors, and is relatively inactive on the α1β2 GABAA receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain.
    6-Methoxyflavanone
  • 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-W015793
    6-Aminonicotinic acid
    		Agonist 99.26%
    6-Aminonicotinic acid is a GABAA receptor agonist with Ki value of 4.4 nM. 6-Aminonicotinic acid can be formed via electrocatalytic synthesis at silver cathodes. 6-Aminonicotinic acid has a variety of biological properties, such as protein synthesis inhibitor, vitamin B3 agonist, and modulating agent in chemotherapy.
    6-Aminonicotinic acid
  • HY-158185
    Isocycloseram
    		Inhibitor 98.16%
    Isocycloseram is an isoxazoline insecticide and acaricide widely recognized as an allosteric modulator of GABA-gated chloride channels. Isocycloseram is active against Lepidopteran, Hemiptera, Coleoptera, Thysanoptera and Diptera pests. Isocycloseram targets the invertebrate Rdl GABA receptor, but the G335M mutation in the third transmembrane domain of the Rdl GABA receptor may mediate resistance.
    Isocycloseram
Cat. No. Product Name / Synonyms Application Reactivity