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-D1704
    Bodipy TMR-X muscimol
    		Agonist 99.79%
    Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations.
    Bodipy TMR-X muscimol
  • HY-105567A
    Carbiphene hydrochloride
    		Antagonist
    Carbiphene hydrochloride is a GABAA receptor allosteric modulator. Carbiphene hydrochloride inhibits [35S] TBPS binding and enhances [3H] muscimol binding on rat forebrain membranes, acting on specific GABAA receptor subsets. Carbiphene hydrochloride can be used in research related to schizophrenia.
    Carbiphene hydrochloride
  • HY-131997
    2'MeO6MF
    		Agonist
    2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
    2'MeO6MF
  • HY-133596
    12,14-Dichlorodehydroabietic acid
    		Antagonist
    12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca2+-activated K+ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca2+ and stimulates transmitter release.
    12,14-Dichlorodehydroabietic acid
  • HY-100783A
    (+)-Bicuculline methochloride
    		Antagonist
    (+)-Bicuculline methobromide is a potent GABAA blocker. (+)-Bicuculline methobromide alters membrane properties and firing pattern. (+)-Bicuculline methobromide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. (+)-Bicuculline methobromide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
    (+)-Bicuculline methochloride
  • HY-W743264
    17β-Estradiol sulfate-d6 sodium
    17β-Estradiol sulfate-d3 sodium (17β-Estradiol 3-sulfate-d3 sodium) is the deuterium labeled 17β-Estradiol sulfate sodium (HY-141672). 17β-Estradiol sulfate sodium, also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.
    17β-Estradiol sulfate-d<sub>6</sub> sodium
  • HY-A0177
    Fominoben
    Fominoben is a type of benzamide-based antitussive agent. Fominoben works by acting on the central nervous system to increase alveolar ventilation, thereby improving the blood oxygen levels in patients with pulmonary diseases (COLD). Fominoben can bind to the benzodiazepine receptor binding sites in the brain and also has anti-anxiety and anti-convulsant effects. Fominoben can be used in research on hypoxemia.
    Fominoben
  • HY-118490
    T-2000
    		Agonist
    T-2000 (DMMDPB) is an orally active GABA receptor agonist with anticonvulsant activities.
    T-2000
  • HY-W777360
    Harman-13C2,15N
    		Inhibitor 99.66%
    Harman-13C2,15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harman-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-173251S
    ENX-101
    		Modulator
    ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.
    ENX-101
  • HY-149400
    GABA-IN-2
    		Inhibitor
    GABA-IN-2 (Compound 5) is a GABA inhibitor. GABA-IN-2 has larvicidal activity and insecticidal effect, with mortality rates of 87% at 50 mg/L.
    GABA-IN-2
  • HY-155305
    BuChE-IN-9
    		Inhibitor
    BuChE-IN-9 (compound 22a) is a potent equine serum-derived BuChE (eqBuChE) inhibitor with an IC50 of 173 nM. BuChE-IN-9 also inhibits human BACE1, Aβ aggregation, mouse GABA transporter 1 (mGAT1) and mGAT4. BuChE-IN-9 has significant antiamnesic properties.
    BuChE-IN-9
  • HY-N2482
    Guvacine
    		Inhibitor
    Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.
    Guvacine
  • HY-120146
    NNC 05-2090
    		Inhibitor
    NNC 05-2090 is aGABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50 sub>: 10.6 μM). NNC 05-2090 also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.
    NNC 05-2090
  • HY-106635
    Suriclone
    		Agonist
    Suriclone (RP31264) is a GABA receptor agonist. Suriclone is an anxiolytic agent with a high affinity for the benzodiazepine receptors. Suriclone has oral activity.
    Suriclone
  • HY-147982
    GABA-AT-IN-1
    GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mouse brain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant.
    GABA-AT-IN-1
  • HY-181135
    Bicyclo-GABA
    		Inhibitor
    Bicyclo-GABA is a selective betaine/GABA transporter 1 (BGT1) competitive, non-transported inhibitor with an IC50 of 590 nM. Bicyclo-GABA exhibits low micromolar agonistic activity at α1β2γ2 GABAA receptors with an EC50 of 5.1 μM. Bicyclo-GABA displays 129 times higher activity for BGT1 than GAT3. Bicyclo-GABA serves as a valuable tool compound for deciphering its elusive pharmacological role in the brain and periphery.
    Bicyclo-GABA
  • HY-118502
    DOV51892
    		Modulator
    DOV51892 is a GABAA receptor modulator. DOV51892 has a specific effect on GABAA receptors containing the α1 subunit. DOV51892 exhibits non-sedative anti-anxiety effects. DOV51892 can be used for in-depth research on the function of GABAA receptors.
    DOV51892
  • HY-116152S
    Cipepofol-d6
    		Activator
    Cipepofol-d6 (Ciprofol-d6; HSK3486-d6) is deuterium labeled Cipepofol (HY-116152). Cipepofol (HSK3486), a psychomotor stabilizing agent, is a gamma-aminobutyric acid (GABA) receptor potentiator.
    Cipepofol-d<sub>6</sub>
  • HY-181552
    GABAA receptor modulator-13
    		Modulator
    GABAA receptor modulator-13 is an orally active, blood-brain barrier-permeable α4β1δ GABAA receptor modulator (IC50 = 9.02 μM). GABAA receptor modulator-13 reduces GABA-induced currents, impairs the stability of the transmembrane domain M2-M3 loop of α4β1δ GABAA receptors, and exhibits selectivity for γ2-containing GABAA receptor subtypes and α6β3δ GABAA receptor subtypes. GABAA receptor modulator-13 is applicable to the research of nervous system diseases with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy.
    GABAA receptor modulator-13
Cat. No. Product Name / Synonyms Application Reactivity