2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

GABA Receptor

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-146099
    GABAA receptor agent 7
    		Inhibitor
    GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy.
    GABAA receptor agent 7
  • HY-N2079A
    (-)-Securinine nitrate
    		Antagonist
    (-)-Securinine nitrate is an alkaloid and also a GABAA receptor antagonist. (-)-Securinine nitrate can be derived from plants.
    (-)-Securinine nitrate
  • HY-146281
    mGAT3/4-IN-2
    		Inhibitor
    mGAT3/4-IN-2 (compound 27b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.44 and 5.25, respectively.
    mGAT3/4-IN-2
  • HY-103524R
    Valerenic acid (Standard)
    		Activator
    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.
    Valerenic acid (Standard)
  • HY-182511
    IUN-00433
    		Activator
    IUN-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.
    IUN-00433
  • HY-105857
    Thiazesim
    		Inhibitor
    Thiazesim is a benzothiazepine compound with a thiophene structure and acts as a GABAA receptor inhibitor, exerting anticonvulsant and antidepressant effects. Thiazesim exhibits specific pharmacological properties in animal experiments. Thiazesim reduces motor activity in rats and effectively inhibits rat killing responses, with a ratio of 2.1 between the ED50 in rotarod tests and the ED50 for anti-killing behavior. Thiazesim can be widely used in basic and clinical studies related to epilepsy.
    Thiazesim
  • HY-103521
    Anxiolytic/nonsedative agent-1
    		Agonist
    Anxiolytic/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.
    Anxiolytic/nonsedative agent-1
  • HY-182023
    Anticonvulsant agent 11
    		Activator
    Anticonvulsant 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.
    Anticonvulsant agent 11
  • HY-100248
    Sarmazenil
    		Antagonist
    Sarmazenil is a benzodiazepine receptor antagonist.
    Sarmazenil
  • HY-118308
    AHN-683
    AHN-683 is a luciferin-derived ligand that targets the peripheral benzodiazepine receptor (BDR).
    AHN-683
  • HY-118844R
    Flumazenil acid (Standard)
    		Antagonist
    Flumazenil acid (Standard) is the analytical standard of Flumazenil acid. This product is intended for research and analytical applications. Flumazenil acid is a metabolite of Flumazenil. Flumazenil is a GABAA receptor antagonist.
    Flumazenil acid (Standard)
  • HY-W743398
    Mexazolam
    Mexazolam (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.
    Mexazolam
  • HY-103498
    Org20599
    		Antagonist
    Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM.
    Org20599
  • HY-182271
    GPR61 Inverse agonist 3
    		Inhibitor
    GPR61 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.
    GPR61 Inverse agonist 3
  • HY-B0696B
    Tiagabine hydrochloride hydrate
    		Inhibitor
    Tiagabine (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.
    Tiagabine hydrochloride hydrate
  • HY-W754627
    Clazolam
    		Modulator
    Clazolam (Isoquinazepon; SAH-1123) is a GABA Receptor modulator. Clazolam can be used in research on neurological diseases.
    Clazolam
  • HY-106044
    Etazolate
    		Modulator
    Etazolate (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.
    Etazolate
  • HY-114040
    NO-711
    		Inhibitor
    NO-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.
    NO-711
  • HY-181961
    SR-THAP
    		Inhibitor
    SR-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.
    SR-THAP
  • HY-139145S
    Etbicyphat-13C3
    Etbicyphat-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.
    Etbicyphat-<sup>13</sup>C<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity