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-N9483R
    7-Keto-DHEA (Standard)
    		Modulator
    7-Keto-DHEA (Standard) (7-Oxo-DHEA (Standard)) is the analytical standard of 7-Keto-DHEA (HY-N9483). This product is intended for research and analytical applications. 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 (Standard)
  • HY-108690R
    Fluxametamide (Standard)
    		Antagonist
    Fluxametamide (Standard) is the analytical standard of Fluxametamide (HY-108690). This product is intended for research and analytical applications. Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
    Fluxametamide (Standard)
  • HY-117106
    PNU-107484A
    PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl- currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes.
    PNU-107484A
  • HY-103534R
    CI-966 hydrochloride (Standard)
    		Inhibitor
    CI-966 hydrochloride (Standard) is the analytical standard of CI-966 hydrochloride (HY-103534). This product is intended for research and analytical applications. 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 (Standard)
  • HY-100800R
    TACA (Standard)
    		Agonist
    TACA (Standard) is the analytical standard of TACA (HY-100800). This product is intended for research and analytical applications. TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.
    TACA (Standard)
  • HY-16579AR
    Etifoxine (Standard)
    		Activator
    Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
    Etifoxine (Standard)
  • HY-101596
    Ethyl dirazepate
    Ethyl dirazepate is a agent which is a benzodiazepine derivative. It has anxiolytic and possibly other characteristic benzodiazepine properties.
    Ethyl dirazepate
  • HY-19065
    Ru-32514
    		Agonist
    Ru-32514 is an agonist of benzodiazepine receptor.
    Ru-32514
  • HY-19250
    U-101017
    		Agonist
    U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects. 
    U-101017
  • HY-103509R
    NNC 05-2090 hydrochloride (Standard)
    		Inhibitor
    NNC 05-2090 hydrochloride (Standard) is the analytical standard of NNC 05-2090 hydrochloride (HY-103509). This product is intended for research and analytical applications. NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.
    NNC 05-2090 hydrochloride (Standard)
  • HY-B0135AR
    Furosemide sodium (Standard)
    		Antagonist
    Furosemide (sodium) (Standard) is the analytical standard of Furosemide (sodium). This product is intended for research and analytical applications. Furosemide sodium is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
    Furosemide sodium (Standard)
  • HY-B0340R
    Nefiracetam (Standard)
    		Activator
    Nefiracetam (Standard) is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.
    Nefiracetam (Standard)
  • HY-W067716R
    Spinacine (Standard)
    		Inhibitor
    Spinacine (Standard) is the analytical standard of Spinacine (HY-W067716). This product is intended for research and analytical applications. 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 (Standard)
  • HY-10232S
    THIP-d4
    		Antagonist
    THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
    THIP-d<sub>4</sub>
  • HY-155381
    APS3
    		Inhibitor
    APS3 is a GABA and nACh receptors inhibitor, with a LC50 of 7.2423 μg/mL against Plutella xylostella.
    APS3
  • HY-W009009R
    L-838417 (Standard)
    		Modulator
    L-838417 (Standard) is the analytical standard of L-838417 (HY-W009009). This product is intended for research and analytical applications. 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 (Standard)
  • HY-124225
    RU 33965
    		Agonist
    RU 33965 is an orally active benzodiazepine receptor weak partial inverse agonist.
    RU 33965
  • 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.
    Insecticidal agent 21
  • HY-107482R
    Picamilon (Standard)
    		Agonist
    Picamilon (Standard) is the analytical standard of Picamilon (HY-107482). This product is intended for research and analytical applications. 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 (Standard)
  • HY-103668AR
    SSD114 hydrochloride (Standard)
    		Agonist
    SSD114 hydrochloride (Standard) is the analytical standard of SSD114 hydrochloride (HY-103668A). This product is intended for research and analytical applications. SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
    SSD114 hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity