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 (786)
Related Products (786)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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DAA-1106
0 ImagesDAA1106 is a peripheral benzodiazepine receptor (PBR) agonist that is permeable to the blood-brain barrier, but has no affinity for GABAA receptors.
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(E) -4-Hydroxycrotonic acid
0 ImagesSynonyms: trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA(E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models.
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Etifoxine hydrochloride
0 ImagesSynonyms: HOE 36-801 hydrochlorideEtifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
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Ornidazole (Levo-)
0 ImagesSynonyms: (S)-Ornidazole; LevornidazoleLevo-ornidazole ((S)-Ornidazole) is the L-isomer of Ornidazole. Ornidazole (Levo-) increases GAD 65/67 expression and decreases brain Glu/GABA ratio. Ornidazole (Levo-) has a mild sedative effect. Levo-ornidazole can be used in the research of anti-anaerobic and anti-parasitic agents.
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Fipronil (Standard)
0 ImagesFipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
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Cholesterol myristate
0 ImagesSynonyms: Cholesteryl myristate; Cholesteryl tetradecanoateCholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
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TP003
0 ImagesTP003 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.
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Alphadolone acetate
0 ImagesCat. No.: HY-108068CAS No.: 23930-37-2Synonyms: Alfadolone acetate; GR 2/1574Alphadolone acetate (Alfadolone acetate) is a steroid agent that can suppress or relieve pain, with antinociception.
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Chlormadinone acetate
0 ImagesChlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders.
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PZ-II-029
0 ImagesPZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects.
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BGT1-IN-1
0 ImagesCat. No.: HY-W033027CAS No.: 406947-32-8BGT1-IN-1 (compound 9) is a potent BGT1 inhibitor with IC50 value of 13.9, 58.3 µM for hBGT1, GAT3, respectively. BGT1-IN-1 shows no cytotoxic. BGT1-IN-1 shows neuroprotective activity.
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Dihydrohonokiol B
0 ImagesSynonyms: DihydrohonokiolDihydrohonokiol B (Dihydrohonokiol) is an anxiolytic agent. Dihydrohonokiol B can reduce the neurotoxicity induced by amyloid β protein by stimulating the GABAC receptor. Dihydrohonokiol B can be used in the research of neurodegenerative diseases such as Alzheimer's disease.
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p-Hydroxybenzaldehyde-d4
0 Imagesp-Hydroxybenzaldehyde-d4 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
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R 29676
0 ImagesR 29676 is a neuroleptic agent and inhibits sodium-dependent GABA binding (GABA uptake).
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Topiramate (Standard)
0 ImagesSynonyms: McN 4853 (Standard); RWJ 17021 (Standard)Topiramate (Standard) is the analytical standard of Topiramate. This product is intended for research and analytical applications. Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
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3-Carene
0 ImagesCat. No.: HY-N6663CAS No.: 13466-78-93-Carene is an orally active TCA cycle enzyme inhibitor. 3-Carene inhibits succinate dehydrogenase and malate dehydrogenase as well as pyruvate kinase, disrupting energy metabolism. 3-Carene disrupts cell wall and cell membrane integrity, leading to potassium ion leakage, protein leakage, membrane depolarization, ATP depletion, morphological disruption, and cell lysis. 3-Carene interferes with amino acid metabolism, pantothenate and CoA biosynthesis, purine and pyrimidine metabolism, and aminoacyl-tRNA biosynthesis. 3-Carene enhances GABA receptor-mediated synaptic responses. 3-Carene can be used in research on bacterial infections, inflammation, anxiety, and sleep disorders.
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4''-Oxoavermectin B1a
0 Images4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.
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Ricinine
0 ImagesRicinine is a central nervous system stimulant found in Ricinus communis. Ricinine binds near the benzodiazepine site of the GABAA receptor, reducing benzodiazepine binding affinity through an allosteric effect, and shows no interaction with AMPA, 5-HT1A, muscarinic receptors, or α1 adrenergic receptors. Ricinine improves memory consolidation in mice at low doses, while at high doses it induces seizures, an effect that is selectively inhibited by diazepam. Ricinine shortens the lifespan of Anopheles mosquitoes through sugar feeding and promotes the development of Plasmodium falciparum in mosquitoes. Ricinine is used in research related to epilepsy, amnesia, and malaria.
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Fluorothyl
0 ImagesSynonyms: Bis(2,2,2-trifluoroethyl) ether; Flurothyl
