2. Vías de señalización
  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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-103503
    CGP13501
    		Modulator 98.01%
    CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol.
    CGP13501
  • HY-19945
    DAA-1106
    		Agonist 99.93%
    DAA1106 is a peripheral benzodiazepine receptor (PBR) agonist that is permeable to the blood-brain barrier, but has no affinity for GABAA receptors.
    DAA-1106
  • HY-103511
    TCS1105
    		99.44%
    TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion.
    TCS1105
  • HY-100370
    MRK-016
    		Antagonist 99.71%
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
    MRK-016
  • HY-118844
    Flumazenil acid
    		Antagonist 99.96%
    Flumazenil acid is a metabolite of Flumazenil. Flumazenil is a GABAA receptor antagonist.
    Flumazenil acid
  • HY-105272
    Loreclezole
    		Agonist 99.97%
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
    Loreclezole
  • HY-115685
    3-Methyl-GABA
    		Activator 99.86%
    3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABAA receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity.
    3-Methyl-GABA
  • HY-B0211R
    Riluzole (Standard)
    		Inhibitor
    Riluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. 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 (Standard)
  • HY-Y0313S
    p-Hydroxybenzaldehyde-d4
    		Antagonist 99.65%
    p-Hydroxybenzaldehyde-d4 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde-d<sub>4</sub>
  • HY-113346S
    Tetrahydrodeoxycorticosterone-d3
    		Agonist 99.53%
    Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.
    Tetrahydrodeoxycorticosterone-d<sub>3</sub>
  • HY-17599
    Piperazine citrate
    		Agonist 98.0%
    Piperazine (1,4-Diazacyclohexane) citrate is a gamma-aminobutyric acid (GABA) agonist. Piperazine citrate is a vital building block and is an essential core in numerous marketed agents with diverse pharmacological activities.
    Piperazine citrate
  • HY-101392A
    Harmane hydrochloride
    		Inhibitor 99.88%
    Harmane hydrochloride 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 hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane hydrochloride
  • HY-113416R
    Dehydroepiandrosterone sulfate (Standard)
    		Antagonist
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate (Standard)
  • HY-137494
    Ethyl β-carboline-3-carboxylate
    		99.75%
    Ethyl β-carboline-3-carboxylate (fl-CCE) is a ligand and short-acting antagonist of benzodiazepine receptors. Ethyl β-carboline-3-carboxylate did not affect cerebellar cGMP levels when used alone, but when taken together with Diazepam, it significantly inhibited the cGMP levels that were upregulated by Diazepam.
    Ethyl β-carboline-3-carboxylate
  • HY-W654100
    Cefepime-d3sulfate
    		Inhibitor 99.50%
    Cefepime-d3 (BMY-28142-d3) sulfate is deuterium labeled Cefepime sulfate. Cefepime sulfate is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime sulfate inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime sulfate penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
    Cefepime-d<sub>3</sub>sulfate
  • HY-B0135S
    Furosemide-d5
    		Antagonist 99.85%
    Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl-?(NKCC) cotransporter, NKCC1 and NKCC2.?Furosemide is also a GABAA?receptors antagonist and displays 100-fold selectivity for?α6-containing receptors than?α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
    Furosemide-d<sub>5</sub>
  • HY-118301
    ADX71441
    		Modulator 98.63%
    ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABAB receptor. ADX71441 potentiates the activity of endogenous GABA at GABAB receptor, with an EC50 of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity.
    ADX71441
  • HY-108295
    Pivagabine
    		Antagonist 98.0%
    Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
    Pivagabine
  • HY-101639A
    CP-409092 hydrochloride
    		Agonist 99.79%
    CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity.
    CP-409092 hydrochloride
  • HY-105791
    Sulazepam
    		99.56%
    Sulazepam, a benzodiazepine, is a selective ovarian cancer G protein-coupled receptor (OGR1) agonist. Sulazepam has anticonvulsive action and has the potential for airway hyperresponsiveness (AHR) research.
    Sulazepam
Cat. No. Nombre del producto / Synonyms Application Reactivity