GABA Receptor
Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid 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.
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GABA Receptor Inhibitors
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GABA Receptor Agonists
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GABA Receptor Antagonists
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GABA Receptor Activators
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GABA Receptor Modulators
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GABA Receptor Controls
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GABA Receptor Ligands
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GABA Receptor Related Products (784)
Related Products (784)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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Tiagabine hydrochloride (Standard)
0 ImagesSynonyms: NO050328 hydrochloride (Standard); NO328 hydrochloride (Standard); TGB hydrochloride (Standard)Tiagabine (hydrochloride) (Standard) is the analytical standard of Tiagabine (hydrochloride). This product is intended for research and analytical applications. Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
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Furosemide hydrochloride
0 ImagesCat. No.: HY-B0135BCAS No.: 42461-27-8Furosemide hydrochloride is an orally active GABAA receptor antagonist. Furosemide hydrochloride inhibits carbonic anhydrase, the sodium-chloride cotransporter, sodium reabsorption, tubuloglomerular feedback, and GABA-induced chloride flux. Furosemide hydrochloride can be used as a diuretic reagent. Furosemide hydrochloride is applied in the research of hepatic necrosis, sepsis-associated acute kidney injury, hypoalbuminemia-related fluid retention, and congestive heart failure.
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5-Deoxykievitone
0 ImagesCat. No.: HY-N15436CAS No.: 74161-24-35-Deoxykievitone, an isoflavanone found in Phaseolus species, is a GABA receptor modulator. 5-Deoxykievitone potentiates GABA-induced chloride current through α1β2γ2s GABAA receptors. 5-Deoxykievitone can be used for the research of epilepsy and anxiety.
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Riluzole hydrochloride (Standard)
0 ImagesSynonyms: PK 26124 hydrochloride (Standard)Riluzole hydrochloride (Standard) is the analytical standard of Riluzole hydrochloride. This product is intended for research and analytical applications. Riluzole hydrochloride 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.
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Gabazine (Standard)
0 ImagesSynonyms: SR95531 (Standard)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.
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Aminooxyacetic acid hemihydrochloride (Standard)
0 ImagesCat. No.: HY-107994RCAS No.: 2921-14-4Synonyms: Carboxymethoxylamine hemihydrochloride (Standard); Aminooxyacetate hemihydrochloride (Standard)Aminooxyacetic acid (hemihydrochloride) (Standard) is the analytical standard of Aminooxyacetic acid (hemihydrochloride). This product is intended for research and analytical applications. Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
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GABA-IN-4
0 ImagesGABA-IN-4 (Compound 17) is a N-(indol-3-ylglyoxylyl)benzylamine derivative. GABA-IN-4 exhibits high affinity for the benzodiazepine receptor (BzR) (binding site in GABAA receptor complex) with Ki value of 67 nM. Benzodiazepines are widely used as antianxiety, sedative-hypnotic and anticonvulsant agents.
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Pipequaline hydrochloride
0 ImagesSynonyms: PK-8165 hydrochloridePipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity.
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Etazolate hydrochloride (Standard)
0 ImagesCat. No.: HY-100936RCAS No.: 35838-58-5Synonyms: SQ 20009 (Standard); EHT 0202 hydrochloride (Standard)Etazolate (hydrochloride) (Standard) is the analytical standard of Etazolate (hydrochloride). This product is intended for research and analytical applications. Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
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(S)-Padsevonil (Standard)
0 ImagesCat. No.: HY-109009ARCAS No.: 1294001-37-8Synonyms: (S)-UCB-0942 (Standard)(S)-Padsevonil (Standard) is the analytical standard of (S)-Padsevonil (HY-109009A). This product is intended for research and analytical applications. (S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
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Riluzole-13C6
0 ImagesCat. No.: HY-B0211S1Synonyms: PK 26124-13C6Riluzole-13C6 (PK 26124-13C6) is 13C labeled Riluzole. 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.
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Padsevonil (Standard)
0 ImagesCat. No.: HY-109009RCAS No.: 1294000-61-5Synonyms: UCB-0942 (Standard)Padsevonil (Standard) is the analytical standard of Padsevonil (HY-109009). This product is intended for research and analytical applications. Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
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CCD-3693
0 ImagesCat. No.: HY-125508CAS No.: 162883-07-0CCD-3693 is an orally active GABA receptor agonist. CCD-3693 has anxiolytic, anticonvulsant and sedative hypnotic activities and can be used in research related to neurological diseases.
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(+)-Kavain (Standard)
0 Images(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
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GBLD345
0 ImagesCat. No.: HY-103535CAS No.: 122479-08-7GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM).
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Oxiracetam (Standard)
0 ImagesSynonyms: ISF2522 (Standard)Oxiracetam (Standard) is the analytical standard of Oxiracetam. This product is intended for research and analytical applications. Oxiracetam (ISF2522) is an orally active and a BBB-penetrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases.
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Pipequaline (Standard)
0 ImagesCat. No.: HY-100140RCAS No.: 77472-98-1Synonyms: PK-8165 (Standard)Pipequaline (Standard) is the analytical standard of Pipequaline. This product is intended for research and analytical applications. Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
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α-Hydroxy etizolam
0 ImagesCat. No.: HY-W705371CAS No.: 64546-10-7α-Hydroxy etizolam is the primary metabolite of Etizolam, possessing nearly identical pharmacological potency and high affinity for benzodiazepine receptors as Etizolam.
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GET73 (Standard)
0 ImagesCat. No.: HY-108034RCAS No.: 202402-01-5GET73 (Standard) is the analytical standard of GET73 (HY-108034). This product is intended for research and analytical applications. GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.
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3-Hydroxymethyl-β-carboline
0 ImagesCat. No.: HY-W197533CAS No.: 65474-79-53-Hydroxymethyl-β-carboline is a Benzodiazepine antagonist with a Ki value of ~1470 nM. 3-Hydroxymethyl-β-carboline reverses Flurazepam-induced sleep, cerebrovascular and cerebral metabolic inhibition, and also partially reverses Flurazepam-induced decreases in blood pressure and heart rate. 3-Hydroxymethyl-β-carboline disrupts the anticonvulsant and anxiolytic effects of Diazepam in male mice. 3-Hydroxymethyl-β-carboline has no effect on sodium-dependent high-affinity choline uptake in rat cortical or hippocampal synaptosomes.
