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-100050
    4-Hydroxymidazolam
    		Modulator
    4-Hydroxymidazolam is a major metabolite of Midazolam. Midazolam is a potent benzodiazepine with anxiolytic properties.
    4-Hydroxymidazolam
  • HY-108035
    (-)-JM-1232
    (-)-JM-1232 (MR04A3) targets GABA A receptors and exerts its analgesic effects by binding to the benzodiazepine binding site of GABA A receptors. (-)-JM-1232 demonstrates potent analgesic effects in mice against acute thermal stimuli, mechanically induced pain, and visceral pain, with CI50 values of 2.96, 3.06, and 2.27 mg/kg, respectively. (-)-JM-1232 can be used in research related to pain and analgesia.
    (-)-JM-1232
  • HY-145257
    GABAA receptor agent 5
    		Antagonist
    GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an Ki of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability.
    GABAA receptor agent 5
  • HY-W742300
    Pipazethate hydrochloride
    		Antagonist
    Pipazethate (SKF 70230A; SQ 15874) hydrochloride is a potent GABA antagonist. Pipazethate hydrochloride shows antitussive activity and can be used in research in cough suppressant .
    Pipazethate hydrochloride
  • HY-125296
    Fipronil sulfone
    		Inhibitor 99.75%
    Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
    Fipronil sulfone
  • HY-100915
    SKF 97541
    		Agonist
    SKF 97541 (CGP 35024) is a potent and selective GABAB agonist that can induce hyperpotential. SKF 97541 has antiepileptic activity.
    SKF 97541
  • HY-167702
    (Rac)-Acetoxyvalerenic acid
    		Modulator
    (Rac)-Acetoxyvalerenic acid is a derivative of valerenic acid that acts as a GABA (A) receptor modulator, potentially providing sedative and sleep-enhancing effects. (Rac)-Acetoxyvalerenic acid exhibits slower permeability across the blood-brain barrier compared to diazepam, indicating that its transport may rely on an unidentified pathway rather than transcellular passive diffusion.
    (Rac)-Acetoxyvalerenic acid
  • 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-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-114871
    SL651498
    		Antagonist
    SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities.
    SL651498
  • HY-124467
    Difludiazepam
    Difludiazepam (Ro 07-4065), a benzodiazepine, has binding affinity (0.613) to GABAA receptors.
    Difludiazepam
  • 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-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-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-B0696B
    Tiagabine hydrochloride hydrate
    		Inhibitor
    Tiagabine hydrochloride hydrate is a potent and selective GABA uptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
    Tiagabine hydrochloride hydrate
  • 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-120970
    Bis(7)-tacrine dihydrochloride
    		Antagonist
    Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .
    Bis(7)-tacrine dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity