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

Related Products

PDF 3.03 MB

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-105481
    CGS-17867A hydrochloride
    		Ligand
    CGS-17867A (hydrochloride) is a benzodiazepine receptor ligand. CGS-17867A (hydrochloride) has a weak sedative effect and can increase palatable food intake.
    CGS-17867A hydrochloride
  • HY-116859
    Ro 14-7437
    		Antagonist
    Ro 14-7437 is a potent and selective potentiating antagonist of Midazolam.
    Ro 14-7437
  • HY-116457
    Propanidid
    		Agonist 98.19%
    Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA) receptor agonist and a short-acting non-barbiturate general agent that can suppress or relieve pain. Propanidid can decrease the arterial pressure.
    Propanidid
  • HY-175670
    GABAA receptor modulator-10
    		Agonist
    GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy.
    GABAA receptor modulator-10
  • HY-117256
    Gabazine free base
    		Antagonist
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of 0.2 μM for GABA receptor.
    Gabazine free base
  • HY-10061A
    Lesogaberan napadisylate
    		Agonist
    Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan napadisylate
  • HY-159826
    Brexanolone caprilcerbate
    		Agonist
    Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator.
    Brexanolone caprilcerbate
  • HY-146280
    mGAT3/4-IN-1
    		Inhibitor
    mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice.
    mGAT3/4-IN-1
  • HY-169432
    TET-13
    		Modulator
    TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively).
    TET-13
  • HY-13694R
    Methionine (Standard)
    		Activator
    Methionine (Standard) is the analytical standard of Methionine. This product is intended for research and analytical applications. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine (Standard)
  • 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-B0355R
    Ginkgolide A (Standard)
    		Antagonist
    Ginkgolide A (Standard) is the analytical standard of Ginkgolide A. This product is intended for research and analytical applications. Ginkgolide A (BN-52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist.
    Ginkgolide A (Standard)
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity