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 Controls
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GABA Receptor Ligands
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GABA Receptor Related Products (777)
Related Products (777)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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2-AEMP
0 ImagesCat. No.: HY-129907CAS No.: 321882-95-5Synonyms: 2-Aminoethyl methylphosphonate2-AEMP (2-Aminoethyl methylphosphonate) is an anti-GABA(A)-ρ1 receptor compound with antagonist activity. 2-AEMP exhibits competitive inhibition compared to TPMPA with an IC(50) value of 18 μM, compared to 7 μM for TPMPA. The release rate of inhibition at termination of 2-AEMP is significantly higher than that of TPMPA. The preincubation time required for the onset of inhibition of 2-AEMP is much shorter than that of TPMPA. Some analogs of 2-AEMP, especially those with benzyl or n-butyl substituents, show lower potency in terms of biological activity.
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Californidine perchlorate
0 ImagesCat. No.: HY-W739289CAS No.: 17939-31-0Californidine perchlorate is an orally active γ-aminobutyric acid (GABA) receptor and serotonin receptor modulator. Californidine perchlorate enhances GABA-mediated chloride influx and inhibits cytochrome P450 enzymes. Californidine perchlorate is promising for research of anxiety.
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BTS 72664
0 ImagesCat. No.: HY-182548CAS No.: 165383-52-8BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABAA receptor (GABAA receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na+ channels (Ki = 350 μM) and NMDA receptors (NMDA receptor) (IC50 = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine.
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Rac-Vigabatrin-13C,d2
0 ImagesCat. No.: HY-W778008CAS No.: 1330171-61-3Rac-Vigabatrin-13C,d2 (Major) is the deuterium and 13C labeled Vigabatrin (HY-15399). Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
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ZL006-05
0 ImagesCat. No.: HY-184108CAS No.: 2486316-20-3ZL006-05 is an orally active, brain-penetrant nNOS–PSD-95 and α2-containing GABAA dual-target inhibitor. ZL006-05 blocks the nNOS-PSD-95 protein-protein interaction and selectively potentiatesα2-containing GABAA receptors. ZL006-05 attenuates central sensitization and strengthens inhibitory GABAergic synaptic transmission. ZL006-05 can be used for the study of neuropathic pain, cancer pain, chemotherapy-induced peripheral neuropathic pain, ischemic stroke, poststroke depression and anxiety.
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3-(4-Chlorophenyl)-4-hydroxybutyric acid sodium
0 ImagesCat. No.: HY-W700174CAS No.: 1346603-21-1
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RP-60503
0 ImagesCat. No.: HY-101643CAS No.: 117705-18-7RP-60503 is an orally active anxiolytic cyclopyrrolone derivative with low sedative potential. RP-60503 binds to the gamma-aminobutyric acidA (GABA)/benzodiazepine receptor with a Ki value of 1.16 nM. RP-60503 can be used for the research of neurological disease.
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CGP 56999
0 ImagesCat. No.: HY-123222CAS No.: 153994-97-9CGP 56999 is a potent antagonist GABA(B) receptor, with the IC50 of 0.002 μM. CGP 56999 increased the levels of BDNF mRNA in the brain in vivo and in vitro.
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GABAA receptor agent 4
0 ImagesCat. No.: HY-145256CAS No.: 2035203-91-7GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential.
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Pregabalin arenacarbil
0 ImagesCat. No.: HY-109156CAS No.: 1174748-30-1Pregabalin arenacarbil is a proagent of Pregabalin.Pregabalin is an analog of gamma-aminobutyric acid (GABA) for the research of post herpetic neuralgia, peripheral diabetic neuropathy,fibromyalgia and epilepsy.
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GABAB receptor antagonist 4
0 ImagesCat. No.: HY-174147CAS No.: 91981-93-0GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases.
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Doxefazepam
0 ImagesSynonyms: SAS-643Doxefazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsan and skeletal muscle relaxant properties.
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RWJ-51204
0 ImagesCat. No.: HY-19308CAS No.: 205701-85-5RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
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NEO 376
0 ImagesSynonyms: SPI-376NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
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CP-457920
0 ImagesCat. No.: HY-118625CAS No.: 220860-50-4CP-457920 (Compound 21) is a GABA receptor inhibitor (Ki ≈ 1 ng/mL). CP-457920 can be used in research on neurological diseases such as Alzheimer's disease.
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Homocarnosine
0 ImagesHomocarnosine is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects.Homocarnosine has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.
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Dehydroepiandrosterone sulfate sodium (Standard)
0 ImagesSynonyms: DHEA sulfate sodium (Standard); Prasterone sulfate sodium (Standard)Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
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Picamilon sodium
0 ImagesCat. No.: HY-107482ACAS No.: 62936-56-5Synonyms: Nicotinoyl-GABA sodium; Nicotinoyl-γ-aminobutyric acid sodiumPicamilon sodium is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon sodium improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.
