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-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-100369A
    DMCM hydrochloride
    		Inhibitor 99.11%
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.
    DMCM hydrochloride
  • HY-N2160
    6'''-Feruloylspinosin
    		99.65%
    6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
    6'''-Feruloylspinosin
  • HY-153584
    MRK-898
    		Modulator 99.48%
    MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s).
    MRK-898
  • HY-103520
    DS2
    		Activator 99.94%
    DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research.
    DS2
  • HY-105056
    Bretazenil
    		Agonist 99.13%
    Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects.
    Bretazenil
  • HY-P2602
    α-Casozepine
    		99.36%
    α-Casozepine is an orally effective anxiolytic that binds to the benzodiazepine site of the GABAA receptor in bovine samples with an IC50 of 88 μM. α-Casozepine exerts anxiolytic and anti-stress effects on cats exposed to unfamiliar environments and dogs undergoing road transport. α-Casozepine exhibits significant anxiolytic activity in rats. α-Casozepine can be used in studies related to fear, anxiety and stress.
    α-Casozepine
  • HY-W009009
    L-838417
    		Modulator 98.73%
    L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2. L-838417 has anti-anxiety activity.
    L-838417
  • HY-129636
    CLH304a
    		Antagonist 99.64%
    CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor.
    CLH304a
  • HY-W105694
    3-Aminopropylphosphonic acid
    		Agonist 98.0%
    3-Aminopropylphosphonic acid ((3-Aminopropyl)phosphonic acid) is a phosphonic acid analogue of GABA and a GABAB receptor agonist.
    3-Aminopropylphosphonic acid
  • HY-B1803A
    Tracazolate hydrochloride
    		Modulator 99.24%
    Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
    Tracazolate hydrochloride
  • HY-N6648
    Cirsimaritin
    		99.88%
    Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin
  • HY-107489
    RO 4938581
    		Antagonist 99.78%
    RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
    RO 4938581
  • HY-W067716
    Spinacine
    		Inhibitor 99.96%
    Spinacine ((S)-Spinacine) is a GABA uptake inhibitor. Spinacine enhances synaptic GABA effects via inhibition of gamma-aminobutyric acid uptake in cerebral cortex slices. Spinacine inhibits reflex responses of ventral roots in isolated spinal cord. Spinacine inhibits motor activity and reduces approaches to water dispensers in conflict situations. Spinacine raises pain sensitivity threshold via subarachnoidal injection.
    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-W101673
    Dipropofol
    		Activator 99.66%
    Dipropofol is an antioxidant agent.
    Dipropofol
  • 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-W677042
    α-Androstenol
    		Activator 99.85%
    α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and male axillary sweat. α-Androstenol is also a positive allosteric modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50 of 0.4 μM). α-Androstenol produces anxiolytic-like, antidepressant-like, and anticonvulsant effects in mice. α-Androstenol can be used for the research of seizures.
    α-Androstenol
  • 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-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.
    4-Acetamidobutanoic acid-d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity