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-B1671R
    (+)-Kavain (Standard)
    (+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
    (+)-Kavain (Standard)
  • HY-103535
    GBLD345
    		Agonist
    GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM).
    GBLD345
  • HY-B1715R
    Oxiracetam (Standard)
    		Agonist
    Oxiracetam (Standard) is the analytical standard of Oxiracetam. This product is intended for research and analytical applications. Oxiracetam (ISF2522) is an orally active and a BBB-penetrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases.
    Oxiracetam (Standard)
  • HY-100140R
    Pipequaline (Standard)
    		Agonist
    Pipequaline (Standard) is the analytical standard of Pipequaline. This product is intended for research and analytical applications. Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline (Standard)
  • HY-W705371
    α-Hydroxy etizolam
    α-Hydroxy etizolam is the primary metabolite of Etizolam, possessing nearly identical pharmacological potency and high affinity for benzodiazepine receptors as Etizolam.
    α-Hydroxy etizolam
  • HY-108034R
    GET73 (Standard)
    GET73 (Standard) is the analytical standard of GET73 (HY-108034). This product is intended for research and analytical applications. GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.
    GET73 (Standard)
  • HY-W197533
    3-Hydroxymethyl-β-carboline
    3-Hydroxymethyl-β-carboline antagonizes the anxiolytic and anticonvulsant actions of Diazepam and reverses the sedative action of Flurazepam. 3-Hydroxymethyl-β-carboline also antagonizes the cerebrovascular and cerebral metabolic depression produced by Flurazepam.
    3-Hydroxymethyl-β-carboline
  • HY-118696
    MGAT2-IN-5
    		Inhibitor
    MGAT2-IN-5 (Compound 17b) is a selective inhibitor for mouse GABA transit protection subsidity 2 (mGAT2) with an IC50 of 45 μM. MGAT2-IN-5 exhibits anticonvulsive efficacy in audiogenic seizure (AGS) susceptible frings mouse model with an ED50 of 20.4 mg/kg.
    MGAT2-IN-5
  • HY-17030R
    Acamprosate calcium (Standard)
    		Agonist
    Acamprosate (calcium) (Standard) is the analytical standard of Acamprosate (calcium). This product is intended for research and analytical applications.
    Acamprosate calcium (Standard)
  • HY-101165R
    Cyclothiazide (Standard)
    		Inhibitor
    Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.
    Cyclothiazide (Standard)
  • HY-100228
    SKF 89976A
    		Inhibitor
    SKF89976A is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
    SKF 89976A
  • HY-171028
    3-Hydroxy desalkylflurazepam
    		Inhibitor
    3-Hydroxy desalkylflurazepam is a benzodiazepine with potential sedative and anxiolytic effects.
    3-Hydroxy desalkylflurazepam
  • HY-186006
    GABRA5 modulator-1
    GABRA5 modulator-1 is a GABRA5 modulator.
    GABRA5 modulator-1
  • HY-B1494R
    Picrotoxinin (Standard)
    		Antagonist
    Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
    Picrotoxinin (Standard)
  • HY-W101673R
    Dipropofol (Standard)
    		Activator
    Dipropofol (Standard) is the analytical standard of Dipropofol. This product is intended for research and analytical applications. Dipropofol is an antioxidant agent.
    Dipropofol (Standard)
  • HY-103474R
    Bicuculline methiodide (Standard)
    		Inhibitor
    Bicuculline methiodide (Standard) is the analytical standard of Bicuculline methiodide (HY-103474). This product is intended for research and analytical applications. Bicuculline methiodide ((-)-Bicuculline methiodide) is a potent GABAA blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
    Bicuculline methiodide (Standard)
  • HY-B0696S1
    Tiagabine-d4
    		Inhibitor
    Tiagabine-d4 (NO050328-d4) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) 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 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 is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
    Tiagabine-d<sub>4</sub>
  • HY-123801A
    MIDD0301 sodium
    		Inhibitor
    MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone (HY-B0214). MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.
    MIDD0301 sodium
  • HY-100369AR
    DMCM hydrochloride (Standard)
    		Inhibitor
    DMCM (hydrochloride) (Standard) is the analytical standard of DMCM (hydrochloride). This product is intended for research and analytical applications. DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively.
    DMCM hydrochloride (Standard)
  • HY-U00228R
    Rilmazafone hydrochloride (Standard)
    Rilmazafone hydrochloride (450191S) is a benzodiazepine (omega) ligand.
    Rilmazafone hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity