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 (795)
Related Products (795)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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Refisolone
0 ImagesCat. No.: HY-172433CAS No.: 202718-04-5Refisolone is an antagonist of the GABAA receptor.
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GMA-839
0 ImagesCat. No.: HY-117955CAS No.: 162882-76-0Synonyms: WAY 141839; Co 2-6749GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics.
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GABAA receptor agent 2 TFA
0 ImagesCat. No.: HY-135482CAS No.: 1781880-44-1GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).
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GABAB receptor antagonist 5
0 ImagesCat. No.: HY-174152GABAB receptor antagonist 5 (Compound 23) is a competitive GABAB receptor antagonist. GABAB receptor antagonist 5 is promising for research of neuropsychiatric diseases, such as epilepsy, depression, and addiction.
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Flupirtine (Standard)
0 ImagesCat. No.: HY-17001ARCAS No.: 56995-20-1Synonyms: D 9998 (Standard)Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
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CGS-9896
0 ImagesCat. No.: HY-103052CAS No.: 77779-36-3CGS-9896 is an orally active benzodiazepine receptor agonist that targets the benzodiazepine receptor allosterically coupled to the GABAA receptor and chloride ion carrier channel. The Ki value of CGS-9896 for benzodiazepine receptors in rats is 0.83 nM. CGS-9896 inhibits pentylenetetrazol-induced convulsions in mice and exerts an anticonvulsant effect.
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Imidazoleacetic acid (Standard)
0 ImagesCat. No.: HY-113413RCAS No.: 645-65-8Synonyms: Imidazolyl-4-acetic acid (Standard)Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity.
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GATT-44
0 ImagesCat. No.: HY-182944CAS No.: 1265900-99-9GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC50 of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated 18F-radiofluorination. The radiolabeled GATT-44 ([18F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases.
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Propofol (Standard)
0 ImagesPropofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
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Pyrazolam
0 ImagesCat. No.: HY-W028389CAS No.: 39243-02-2Pyrazolam is a brominated triazolo benzodiazepine psychoactive substance with oral effectiveness. Pyrazolam produces anxiolytic, sedative, and sleep-promoting effects. Pyrazolam can be used for the research of anxiety.
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p-Hydroxybenzaldehyde-d5
0 ImagesCat. No.: HY-Y0313S2CAS No.: 298704-22-0p-Hydroxybenzaldehyde-d5 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
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Ro 22-8515
0 ImagesCat. No.: HY-111194CAS No.: 89052-67-5Ro 22-8515 is a ligand of Benzodiazepine receptor.
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Brallobarbitone
0 ImagesCat. No.: HY-W742312CAS No.: 561-86-4Synonyms: UcedormBrallobarbitone is a positive allosteric modulator of GABAA receptor. Brallobarbitone can be used in the research of β-cell dysfunction.
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U-89843A
0 ImagesSynonyms: PNU-89843U-89843A (PNU-89843) is a GABAA receptors positive allosteric modulator (PAM). U-89843A enhances GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A shows antioxidant and sedative effects.
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Denzimol
0 ImagesCat. No.: HY-105059CAS No.: 73931-96-1Denzimol is an orally active anticonvulsant agent. Denzimol inhibits cytochrome P450, and interacts with benzodiazepine receptors. Denzimol selectively antagonizes tonic components of Metrazol-induced seizures in rats and mice. Denzimol can be used for the research of epilepsy and convulsions.
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UMB68 sodium
0 ImagesCat. No.: HY-135034CAS No.: 581099-89-0UMB68 sodium is a selective GHB receptor ligand. UMB68 sodium displaces [3H]NCS-382 with an IC50 of 38 nM in rat cerebrocortical membranes. UMB68 sodium has no significant affinity at GABAB receptors, cannot be metabolized to GABA-active compounds.
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GABAA receptor agonist 2
0 ImagesCat. No.: HY-147736GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression.
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NAP-1
0 ImagesCat. No.: HY-156061CAS No.: 131721-28-3
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GABAA receptor modulator-9
0 ImagesCat. No.: HY-175251GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype GABAA that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC50: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC50s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE).
