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 (788)
Related Products (788)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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CGS 8216
0 ImagesCGS 8216 is a non-benzodiazepine brain benzodiazepine receptor ligand that binds to rat forebrain membranes with high affinity and specificity. CGS 8216 also inhibits 3H-flunitrazepam (3H-FLU) binding to rat synaptosomal membranes and blocks 3H-FLU labeling of brain benzodiazepine receptors in vivo with potency equivalent to Diazepam.
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Cinazepam
0 ImagesCinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.
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Cefepime-d8 sulfate
0 ImagesCefepime-d8 (BMY-28142-d8) sulfate is deuterium labeled Cefepime sulfate. Cefepime sulfate is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime sulfate inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime sulfate penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
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Cefepime Dihydrochloride Monohydrate (Standard)
0 ImagesCefepime (BMY-28142) Dihydrochloride Monohydrate (Standard) is the analytical standard of Cefepime Dihydrochloride Monohydrate. This product is intended for research and analytical applications. Cefepime Dihydrochloride Monohydrate is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime Dihydrochloride Monohydrate inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime Dihydrochloride Monohydrate penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
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NS11394
0 ImagesNS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
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Arecaidine hydrobromide
0 ImagesArecaidine hydrobromide is a GABA transport system inhibitor. Arecaidine hydrobromide inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrobromide inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrobromide inhibits hPAT1-mediated L-[3H]proline uptake in cells. Arecaidine hydrobromide can be used in research related to neurological diseases.
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β-CCM
0 ImagesSynonyms: Beta-CCM; Ro 22-7497β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and proconvulsant effects. β-CCM enhances emotional reactivity and reduces vulnerability to interference in spatial working memory tasks. β-CCM can be used for research on anxiety-related disorders.
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6-Hydroxyflavanone
0 Images6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes.
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Fipronil-13C6
0 ImagesCat. No.: HY-B0822S1Purity: 98%Fipronil-13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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ONO-8590580
0 ImagesONO-8590580 is a GABAA α5 negative allosteric modulator.
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SJM-3
0 ImagesCat. No.: HY-131941CAS No.: 1234977-97-9SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.
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NCS-382 sodium
0 ImagesNCS-382 (sodium) is a potent GABA receptor antagonist. NCS-382 (sodium) has anti-sedative and anti-hypnotic activities and can be used in research related to neurological diseases.
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Thiomuscimol
0 ImagesCat. No.: HY-129927CAS No.: 62020-54-6Thiomuscimol is a GABAA receptor agonist (IC50=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
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4-Acetamidobutanoic acid (Standard)
0 ImagesSynonyms: N-acetyl GABA (Standard)Josamycin propionate (Standard) is the analytical standard of Josamycin propionate. This product is intended for research and analytical applications. Josamycin propionate is classified as a macrolide antibiotic.
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Alphadolone
0 ImagesSynonyms: AlfadoloneAlphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia.
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Pagoclone
0 ImagesCat. No.: HY-101665CAS No.: 133737-32-3Synonyms: (+)-RP-59037; IP-456; RP-62955Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.
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Harman-13C2,15N
0 ImagesCat. No.: HY-W777360CAS No.: 1189461-56-0Harman-13C2,15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
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(E/Z)-CLH304a
0 ImagesCat. No.: HY-129636ACAS No.: 797-17-1Synonyms: GABAB receptor antagonist 1(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors.
