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

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114706
    Suritozole
    Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on GABAA ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases.
    Suritozole
  • HY-103505R
    CL 218872 (Standard)
    Modulator
    CL 218872 (Standard) is the analytical standard of CL 218872 (HY-103505). This product is intended for research and analytical applications. CL 218872 is an orally active and selective ligand for the benzodiazepine receptor subtype BZ1. CL 218872 exhibits anxiolytic, sedative and anticonvulsant activities. CL 218872 can be used in researches of anxiety related disorders and epilepsy.
    CL 218872 (Standard)
  • HY-139226
    GMQ
    Antagonist
    GMQ is an acid-sensing ion channel modulator, competitive GABAAR antagonist. GMQ preferentially, potently, competitively inhibits GABAARs. GMQ inhibits α1β2, α1β2γ2, α4β2γ2 and α5β2γ2 GABAARs. GMQ enhances neuronal excitation through inhibition of GABAergic transmission. GMQ has anti-histamine effects in the enteric system, inhibiting gastric acid secretion.
    GMQ
  • HY-100810R
    Isoguvacine hydrochloride (Standard)
    Agonist
    Isoguvacine (hydrochloride) (Standard) is the analytical standard of Isoguvacine (hydrochloride) (HY-100810). This product is intended for research and analytical applications. Isoguvacine hydrochloride is a GABA receptor agonist.
    Isoguvacine hydrochloride (Standard)
  • HY-160105
    GABAB receptor antagonist 3
    Antagonist
    GABAB receptor antagonist 3 (example 3) is a antagonist of GABAB receptor.
    GABAB receptor antagonist 3
  • HY-136942
    DS1
    Agonist
    DS1 is a potent GABAA agonist. DS1 increases the activity of serum response element (SRE) and cAMP response element (CRE) promoters. DS1 induces luteinizing hormone beta (LHbeta) and follicle-stimulating hormone beta (FSHbeta) promoter activity.
    DS1
  • HY-167658
    Tuclazepam
    Tuclazepam (KC 1956) is a derivative of benzodiazepines that has anti-anxiety and sedative effects.
    Tuclazepam
  • HY-129710
    CGP47656
    Agonist
    CGP47656 is a potent GABAB receptor agonist that inhibits Forskolin (HY-15371)-stimulated adenylyl cyclase activity and augments noradrenaline-stimulated adenylyl cyclase activity. CGP47656 is promising for research of brain function-related diseases.
    CGP47656
  • HY-101059R
    FGIN 1-27 (Standard)
    Agonist
    FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27. This product is intended for research and analytical applications. FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions.
    FGIN 1-27 (Standard)
  • HY-W765182
    Emamectin-d3
    Agonist
    Emamectin-d3 is the deuterium labeled Emamectin. Emamectin is a macrocyclic lactone insecticide. Emamectin acts as agonist for GABA-gated chloride channels.
    Emamectin-d<sub>3</sub>
  • HY-14856
    Atagabalin
    Agonist
    Atagabalin (PD 0200390) is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety and sedative effects. Atagabalin enhances the activity of the GABA receptor by binding to the α2δ subunit of the GABA receptor, thereby increasing the GABA mediated inhibition. This enhancement results in reduced excitability of neurons, helping to reduce anxiety and improve sleep. Atagabalin can be used to study neuropsychiatric disorders, anxiety or sleep disorders.
    Atagabalin
  • HY-103528R
    SCS (Standard)
    Inhibitor
    SCS (Standard) is the analytical standard of SCS (HY-103528). This product is intended for research and analytical applications. SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions.
    SCS (Standard)
  • HY-17354A
    (R)-Baclofen hydrochloride
    Agonist 98.12%
    (R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist.
    (R)-Baclofen hydrochloride
  • HY-108403R
    Phenibut (Standard)
    Agonist
    Phenibut (Standard) is the analytical standard of Phenibut (HY-108403). This product is intended for research and analytical applications. Phenibut (β-Phenyl-GABA) is a GABA-B agonist. Phenibut acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut has anxiolytic and nootropic (cognition enhancing) effects.
    Phenibut (Standard)
  • HY-121877S
    Valnoctamide-d5
    Valnoctamide-d5 is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors.
    Valnoctamide-d<sub>5</sub>
  • HY-121618R
    α-Thujone (Standard)
    Modulator
    α-Thujone (Standard) is the analytical standard of α-Thujone. This product is intended for research and analytical applications. α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
    α-Thujone (Standard)
  • HY-N6648R
    Cirsimaritin (Standard)
    Cirsimaritin (Standard) is the analytical standard of Cirsimaritin (HY-N6648). This product is intended for research and analytical applications. Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin (Standard)
  • HY-111052R
    AZD7325 (Standard)
    Agonist
    AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
    AZD7325 (Standard)
  • HY-B1326R
    Bemegride (Standard)
    Antagonist
    Bemegride (Standard) is the analytical standard of Bemegride. This product is intended for research and analytical applications. Bemegride (3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
    Bemegride (Standard)
  • HY-N1951R
    Miltirone (Standard)
    Agonist
    Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).
    Miltirone (Standard)
Cat. No. Product Name / Synonyms Application Reactivity