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 (789)
Related Products (789)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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Valerenic acid (Standard)
0 ImagesCat. No.: HY-103524RCAS No.: 3569-10-6Synonyms: (-)-Valerenic Acid (Standard)Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.
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IUN-00433
0 ImagesCat. No.: HY-182511CAS No.: 2188230-70-6IUN-00433 (Compound 36) is a selective positive allosteric modulator of α4β1δ-type GABAA receptors, with an EC50 of 0.060 μM. IUN-00433 is applicable to research related to neurological disorders.
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Thiazesim
0 ImagesThiazesim is a CNS-penetrant GABAA receptor inhibitor, exerting anticonvulsant and antidepressant effects. Thiazesim depresses amygdala output, disrupts conditioned avoidance response in rats. Thiazesim can be used for the research of depression and epilepsy.
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Anxiolytic/nonsedative agent-1
0 ImagesCat. No.: HY-103521CAS No.: 355022-97-8Anxiolytic/nonsedative agent-1 (compound 2b) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.
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Anticonvulsant agent 11
0 ImagesCat. No.: HY-182023Anticonvulsant agent 11 (Compound 8b) is an anticonvulsant agent. Anticonvulsant agent 11 exerts neuroprotective effects by enhancing cell viability and reducing ROS levels. Anticonvulsant agent 11 induces the expression of GABAA α1, resulting in neuronal hyperpolarization. Anticonvulsant agent 11 increases the number of neurite-bearing cells and the length of neurites. Anticonvulsant agent 11 exhibits dose-dependent anticonvulsant effects in mice. Anticonvulsant agent 11 can be used for the research of epilepsy.
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Sarmazenil
0 ImagesCat. No.: HY-100248CAS No.: 78771-13-8Synonyms: Ro 15-3505Sarmazenil is a benzodiazepine receptor antagonist.
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AHN-683
0 ImagesCat. No.: HY-118308CAS No.: 143934-15-0AHN-683 is a luciferin-derived ligand that targets the peripheral benzodiazepine receptor (BDR).
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Mexazolam
0 ImagesCat. No.: HY-W743398CAS No.: 31868-18-5Synonyms: CS-386Mexazolam (CS-386) is an orally active benzodiazepine and anxiolytic. Benzodiazepines bind to specific BZD-type receptors on the GABA-chloride complex and potentiate the inhibitory effects of GABA.
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Org20599
0 ImagesCat. No.: HY-103498CAS No.: 156685-94-8Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM.
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EF1500
0 ImagesCat. No.: HY-189042CAS No.: 738562-57-7EF1500 is a potent human GABA transporter 1 (hGAT1) inhibitor and a lipophilic THPO analog. EF1500 occupies the binding site by forming a hydrogen bond with active residues of hGAT1 (such as Tyr139) through its exocyclic amino group, thereby blocking GABA reuptake. EF1500 can be used for research on central nervous system diseases.
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GPR61 Inverse agonist 3
0 ImagesCat. No.: HY-182271GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia.
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Tiagabine hydrochloride hydrate
0 ImagesCat. No.: HY-B0696BCAS No.: 145821-57-4Synonyms: NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrateTiagabine (NO050328; NO328; TGB) hydrochloride hydrate 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 hydrate 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 hydrate 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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Clazolam
0 ImagesCat. No.: HY-W754627CAS No.: 7492-29-7Synonyms: Isoquinazepon; SAH-1123Clazolam (Isoquinazepon; SAH-1123) is a GABA Receptor modulator. Clazolam can be used in research on neurological diseases.
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Etazolate
0 ImagesCat. No.: HY-106044CAS No.: 51022-77-6Synonyms: SQ 64442Etazolate (SQ 64442) is a α-secretase activator, selective PDE4 inhibitor, selective GABAA receptor modulator. Etazolate reduces IL-1β levels Etazolate exerts a dose-dependent anti-inflammatory and anti-œdematous effect accompanied by lasting memory improvement. Etazolate produces an antidepressant-like effect.
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NO-711
0 ImagesCat. No.: HY-114040CAS No.: 159094-94-7Synonyms: NNC-711 free acidNO-711 (NNC-711) free acid is a novel potent and selective inhibitor of γ-aminobutyric acid uptake. NO-711 inhibits synaptosomal (IC50 = 47 nM), neuronal (IC50 = 1238 nM) and glial (IC50 = 636 nM) GABA uptake in vitro.
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SR-THAP
0 ImagesCat. No.: HY-181961CAS No.: 3098361-74-8SR-THAP is a γ-aminobutyric acid transporter 3 (GAT3) inhibitor with an IC50 of 4.9 μM, and exhibits 42-fold and 23-fold selectivity over GAT1 and GlyT1, respectively. SR-THAP inhibits GABA uptake in mammalian cells. SR-THAP is applicable to the research of epilepsy, Alzheimer's disease and ischemic stroke.
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Etbicyphat-13C3
0 ImagesCat. No.: HY-139145SCAS No.: 2300178-69-0Synonyms: Trimethylopropane phosphate-13C3Etbicyphat-13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors.
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Nitrazolam
0 ImagesNitrazolam is a benzodiazepine compound, that may exhibit CNS depressant properties as traditional benzodiazepines, including sedation, hypnosis, anxiolysis, and anticonvulsant effects, by acting on GABA receptors.
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Vigabatrin-13C,d2 hydrochloride
0 ImagesCat. No.: HY-B0033SSynonyms: γ-Vinyl-GABA-13C,d2 hydrochlorideVigabatrin-13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride 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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β-CCB
0 ImagesCat. No.: HY-100924CAS No.: 84454-35-3β-CCB is a ligand for benzodiazepine receptor, which inhibits the binding of [3H]flunitrazepam and ethyl (3-[3H]carboline-3-carboxylate to benzodiazepine receptors, with Ki of 3-4 nM. β-CCB exhibits proconvulsant and anxiogenic effects.
