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-107782R
    Picrotin (Standard)
    Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission.
    Picrotin (Standard)
  • HY-W709349
    Flupirtine hydrochloride
    		Activator
    Flupirtine (D 9998) hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride 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 hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
    Flupirtine hydrochloride
  • HY-165444
    CP-615003
    		Agonist
    CP-615003 is a potent and subtype-selective partial agonist of GABAA receptor (GABAA receptor) (Ki = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABAA receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications.
    CP-615003
  • HY-139145
    Etbicyphat
    		Antagonist 98.0%
    Etbicyphat (Trimethylopropane phosphate) 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
  • HY-119605
    DAA-1097
    		Agonist
    DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects.
    DAA-1097
  • HY-N0662R
    Amentoflavone (Standard)
    		Modulator
    Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.
    Amentoflavone (Standard)
  • HY-106851
    Panadiplon
    		Agonist
    Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.
    Panadiplon
  • HY-105857A
    Thiazesim hydrochloride
    Thiazesim hydrochloride is a benzothiazepine compound with a thiophene structure and acts as a GABAA receptor inhibitor, exerting anticonvulsant and antidepressant effects. Thiazesim hydrochloride exhibits specific pharmacological properties in animal experiments. Thiazesim hydrochloride 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 hydrochloride can be widely used in basic and clinical studies related to epilepsy.
    Thiazesim hydrochloride
  • HY-177573
    Cholesteryl γ-aminobutyrate
    Cholesteryl γ-aminobutyrate is a γ-aminobutyric acid (GABA)-mimetic prodrug. Cholesteryl γ-aminobutyrate inhibits the orthodromically-evoked discharge of pyramidal cells in the CA1 region of the hippocampus. Cholesteryl γ-aminobutyrate suppresses the open-field activity of mice and rats in a dose-dependent manner and inhibits Bicuculline (HY-N0219)-induced seizures in mice. Cholesteryl γ-aminobutyrate can be used for the study of CNS diseases related to impaired GABAergic neuronal function.
    Cholesteryl γ-aminobutyrate
  • HY-W722556
    5α-Androstan-3α-ol
    		Agonist
    5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms.
    5α-Androstan-3α-ol
  • HY-P5860
    MmTx1 toxin
    		Modulator
    MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor susceptibility to agonist.
    MmTx1 toxin
  • HY-103518
    CGP36216
    		Antagonist
    CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders.
    CGP36216
  • HY-177099
    Lorotomidate
    		Agonist
    Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED50: i.v., 2 mg/kg in KM mice; LD50: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.
    Lorotomidate
  • HY-118018
    CHF-2993
    		Inhibitor
    CHF-2993 is an orally active anticonvulsant. CHF-2993 antagonizes Bicuculline (HY-N0219)- and Picrotoxin (HY-101391)-induced tonic convulsions in mice, shows no activity against Pentylenetetrazole-induced clonic convulsions in mice, and partially reduces Veratridine (HY-N6691)-induced aspartate efflux in rat cortical synaptosomes. CHF-2993 can be used in the research of epilepsy.
    CHF-2993
  • HY-119105
    LY81067
    LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites.
    LY81067
  • HY-103513
    GABAA receptor agent 2
    		Modulator
    GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
    GABAA receptor agent 2
  • HY-19438
    Divaplon
    		Agonist
    Divaplon is a GABA receptor agonist with the EC50 values of 31 and 2 nM for α3β2γ2 and α5β2γ2, respectively. Divaplon shows anxiolytic activity.
    Divaplon
  • HY-146100
    GABAA receptor agent 8
    		Inhibitor
    GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy.
    GABAA receptor agent 8
  • HY-123240
    CI-966
    		Inhibitor
    CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities.
    CI-966
  • HY-111298
    TG 41
    		Modulator
    TG 41 is positive modulator of GABAA receptor. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes.
    TG 41
Cat. No. Product Name / Synonyms Application Reactivity