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-111136
    BL-1020 mesylate
    		Agonist
    BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate.
    BL-1020 mesylate
  • HY-14856A
    iso-Atagabalin hydrochloride
    		Agonist
    iso-Atagabalin (iso-PD 0200390) hydrochloride is a stereoisomer of Atagabalin (HY-14856). Atagabalin is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety effect.
    iso-Atagabalin hydrochloride
  • HY-129408
    SGE-516
    		Modulator
    SGE-516 is a neuroactive steroid that is a potent positive allosteric modulator of synaptic and extra-synaptic GABAA receptors. SGE-516 has anticonvulsant activity.
    SGE-516
  • HY-10233R
    Gaboxadol hydrochloride (Standard)
    		Modulator
    Gaboxadol (hydrochloride) (Standard) is the analytical standard of Gaboxadol (hydrochloride). This product is intended for research and analytical applications. Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.
    Gaboxadol hydrochloride (Standard)
  • HY-N15001
    Gabaculine
    		Inhibitor
    Gabaculine is found in the strain of Streptomyces toyocaensis. Gabaculine inhibits GABA aminotransferase.
    Gabaculine
  • HY-W028263
    6-Hydroxyflavanone
    		Inhibitor
    6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes.
    6-Hydroxyflavanone
  • HY-16579R
    Etifoxine hydrochloride (Standard)
    		Activator
    Etifoxine (hydrochloride) (Standard) is the analytical standard of Etifoxine (hydrochloride). This product is intended for research and analytical applications. Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
    Etifoxine hydrochloride (Standard)
  • HY-106437
    ELB-139
    		Agonist
    ELB-139 is a progesterone analogue. ELB-139 is a GABAA receptor partial agonist. ELB-139 has anxiolytic and anticonvulsant activity. ELB-139 induces increase of extracellular 5-HT in the striatum and the medial prefrontal cortex of rats.
    ELB-139
  • HY-69359R
    Nipecotic acid (Standard)
    		Inhibitor
    Nipecotic acid (Standard) is the analytical standard of Nipecotic acid. This product is intended for research and analytical applications. Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM.
    Nipecotic acid (Standard)
  • HY-135154
    epi-Aszonalenin A
    epi-Aszonalenin A is a benzodiazepine fungal metabolite originally isolated from Aspergillus novofumigatus. epi-Aszonalenin A can be used as a psychoactive agent.
    epi-Aszonalenin A
  • HY-U00241
    Carburazepam
    Carburazepam is a agent which derives from benzodiazepine. Benzodiazepines (BZD, BZs) are a class of psychoactive agents whose core chemical structure is the fusion of a benzene ring and a diazepine ring.
    Carburazepam
  • HY-U00102
    Suclofenide
    Suclofenide (Neosulfalepsine; PB385) is an anticonvulsant that affects GABA metabolism.
    Suclofenide
  • HY-U00192
    CGP11952
    CGP11952 is a triazolyl-Benzaphenon resembling the benzodiazepines in its pharmacological action. CGP11952 is an experimental benzodiazepine derivative.
    CGP11952
  • HY-U00215
    Ro 41-3290
    		Agonist
    Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the benzodiazepine receptor.
    Ro 41-3290
  • HY-U00233
    FG8119
    		Agonist
    FG8119 is a novel benzodiazepine agonist extracted from patent US 4745112 A.
    FG8119
Cat. No. Product Name / Synonyms Application Reactivity