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-100810
    Isoguvacine hydrochloride
    		Agonist 99.81%
    Isoguvacine hydrochloride is a GABA receptor agonist.
    Isoguvacine hydrochloride
  • HY-103530
    CGP35348
    		Antagonist ≥98.0%
    CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.
    CGP35348
  • HY-B1671
    (+)-Kavain
    		99.98%
    (+)-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
  • HY-B0837
    Emamectin Benzoate
    		Activator 98.39%
    Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. Emamectin Benzoate is one of semi-synthetic derivative of Avermectin (HY-15311) with a broadspectrum of insecticidal and acaricidal activity. Emamectin Benzoate induces ROS-mediated DNA damage and cell apoptosis. Emamectin Benzoate, a mixture of the natural Emamectin B1a benzoate and Emamectin B1b benzoate, has the main component of Emamectin B1a benzoate.
    Emamectin Benzoate
  • HY-N0700
    alpha-Asarone
    		Activator 99.88%
    alpha-Asarone (α-Asarone) is one of the main psychoactive compounds, and possesses an antidepressant-like activity in mice.
    alpha-Asarone
  • HY-103474
    Bicuculline methiodide
    		Inhibitor 99.24%
    Bicuculline methiodide is a potent GABA(A) receptors 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
  • HY-B0355
    Ginkgolide A
    		Antagonist ≥98.0%
    Ginkgolide A (BN-52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist.
    Ginkgolide A
  • HY-120051
    Afizagabar
    		Antagonist 98.40%
    Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy.
    Afizagabar
  • HY-116152
    Cipepofol
    		Agonist 99.82%
    Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis.
    Cipepofol
  • HY-16716
    Basmisanil
    		Inhibitor 99.91%
    Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.
    Basmisanil
  • HY-120874
    PF-06372865
    		Activator 99.29%
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.
    PF-06372865
  • HY-14426
    L-655708
    		Inhibitor 99.92%
    L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
    L-655708
  • HY-B0927
    Hydrastine
    		Control 99.96%
    Hydrastine is a natural alkaloid found in Hydrastis canadensis and other plants of the Ranunculaceae family.
    Hydrastine
  • HY-103516
    CGP55845 hydrochloride
    		Antagonist ≥99.0%
    CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC50 of 6 nM. CGP55845 hydrochloride can be used for neurological research.
    CGP55845 hydrochloride
  • HY-10233
    Gaboxadol hydrochloride
    		Modulator 99.85%
    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
  • HY-N0067S1
    γ-Aminobutyric acid-d2
    		Agonist 99.72%
    γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
    γ-Aminobutyric acid-d<sub>2</sub>
  • HY-141672
    17β-Estradiol sulfate sodium
    		≥99.0%
    17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.
    17β-Estradiol sulfate sodium
  • HY-B0822
    Fipronil
    		Antagonist 98.98%
    Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
    Fipronil
  • HY-14840
    Phenylpiracetam
    		Activator 99.91%
    Phenylpiracetam(Phenotropyl; Phenotropil) is a phenylated derivative of the nootropic drug piracetam.
    Phenylpiracetam
  • HY-101392
    Harmane
    		Inhibitor 99.91%
    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 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).
    Harmane
Cat. No. Product Name / Synonyms Application Reactivity