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. 상품명 효과 Purity Chemical Structure
  • HY-109009AR
    (S)-Padsevonil (Standard)
    		Modulator
    (S)-Padsevonil (Standard) is the analytical standard of (S)-Padsevonil (HY-109009A). This product is intended for research and analytical applications. (S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
    (S)-Padsevonil (Standard)
  • HY-B0211S1
    Riluzole-13C6
    		Inhibitor
    Riluzole-13C6 (PK 26124-13C6) is 13C labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
    Riluzole-<sup>13</sup>C<sub>6</sub>
  • HY-109009R
    Padsevonil (Standard)
    Padsevonil (Standard) is the analytical standard of Padsevonil (HY-109009). This product is intended for research and analytical applications. Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
    Padsevonil (Standard)
  • HY-125508
    CCD-3693
    		Agonist
    CCD-3693 is an orally active GABA receptor agonist. CCD-3693 has anxiolytic, anticonvulsant and sedative hypnotic activities and can be used in research related to neurological diseases.
    CCD-3693
  • 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 is a Benzodiazepine antagonist with a Ki value of ~1470 nM. 3-Hydroxymethyl-β-carboline reverses Flurazepam-induced sleep, cerebrovascular and cerebral metabolic inhibition, and also partially reverses Flurazepam-induced decreases in blood pressure and heart rate. 3-Hydroxymethyl-β-carboline disrupts the anticonvulsant and anxiolytic effects of Diazepam in male mice. 3-Hydroxymethyl-β-carboline has no effect on sodium-dependent high-affinity choline uptake in rat cortical or hippocampal synaptosomes.
    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)
Cat. No. 상품명 / Synonyms Application Reactivity