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-116702
    Flufiprole
    		Inhibitor
    Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests.
    Flufiprole
  • HY-170930
    Anticonvulsant agent 9
    		Activator
    Anticonvulsant agent 9 (compound 4f) is an α1β2γ2 GABAA receptors activator. Anticonvulsant agent 9 activatesα1β2γ2 GABAA receptors with an EC50 of 1.24 μM. Anticonvulsant agent 9 inhibits the inactivation of Nav1.2 channels. Anticonvulsant agent 9 exhibits significant anticonvulsant activities.
    Anticonvulsant agent 9
  • HY-109077S
    Tigolaner-d4
    		Antagonist
    Tigolaner-d4 is deuterium labeled Tigolaner. Tigolaner (BAY-1272858) acts on γ-aminobutyric acid (GABA) and glutamate-gated chloride channels. Tigolaner has antiparasitic activity.
    Tigolaner-d<sub>4</sub>
  • HY-118931
    EF-1502
    EF-1502 is a potent and selective GABA transporter inhibitor with GAT1 and BGT1 inhibitory activity. EF-1502 produces a synergistic anti-epileptic effect when used in combination with Tiagabine (HY-B0696), a compound used to suppress epileptic seizures. The dosing combination of EF-1502 exhibited reduced anti-epileptic efficacy and dyskinesia when used with THIP (HY-10232). The mechanism of EF-1502 differs significantly from Tiagabine, suggesting a unique role in the inhibitory strategy.
    EF-1502
  • HY-158252S
    Tiagabine-d5 (hydrochloride)
    		Inhibitor
    Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
    Tiagabine-d<sub>5</sub> (hydrochloride)
  • HY-103500
    Ro19-4603
    		Inhibitor
    Ro19-4603 is a benzodiazepine inverse agonist. Ro19-4603 antagonizes ethanol (EtOH) intake in alcohol-preferring rats.
    Ro19-4603
  • HY-116910
    CPP-115
    		Inhibitor
    CPP-115 is a GABA transaminase inactivator with higher affinity and lower retinal toxicity than Vigabatrin (HY-15399). CPP-115 increases brain GABA levels by inhibiting GABA transaminase catabolism. CPP-115 can be used in the study of drug addiction and infantile spasms.
    CPP-115
  • HY-105627A
    Profadol hydrochloride
    		Agonist
    Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR.
    Profadol hydrochloride
  • HY-N0219R
    Bicuculline (Standard)
    		Antagonist
    Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice.
    Bicuculline (Standard)
  • HY-103518A
    CGP36216 hydrochloride
    		Antagonist
    CGP36216 hydrochloride is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders.
    CGP36216 hydrochloride
  • HY-103225
    S-8510 phosphate
    		Antagonist
    S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.
    S-8510 phosphate
  • HY-N0042R
    Ginsenoside Rc (Standard)
    		Agonist
    Ginsenoside Rc (Standard) is the analytical standard of Ginsenoside Rc. This product is intended for research and analytical applications. Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
    Ginsenoside Rc (Standard)
  • HY-100124
    Bamaluzole
    		Agonist
    Bamaluzole is a GABA receptor agonist extracted from patent WO 2012064642 A1.
    Bamaluzole
  • HY-106670
    Dulozafone
    		Activator
    Dulozafone (F1933) shows anticonvulsant activity and can be used for epilepsy research.
    Dulozafone
  • HY-111481
    Flutazolam
    Flutazolam (MS 4101; Ro 7-6102) is a medicine acts on benzodiazepine receptors of the brain and relieves anxiety or tension.
    Flutazolam
  • HY-129105A
    Chlormethiazole (edisylate)
    Chlormethiazole (edisylate) is a sedative-hypnotic with active allosteric modulatory activity at GABAA receptors.
    Chlormethiazole (edisylate)
  • HY-B0007S2
    Baclofen-d5 hydrochloride
    		Agonist
    Baclofen-d5 hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
    Baclofen-d<sub>5</sub> hydrochloride
  • HY-168977
    Inidascamine
    		Modulator
    Inidascamine is the modulator for cholinergic, glutamatergic, and GABAB receptor, and can be used for researchs of schizophrenia.
    Inidascamine
  • HY-123301
    GABAB receptor antagonist 2
    		Antagonist
    GABAB receptor antagonist 2 is a GABAB receptor/b> antagonist.
    GABAB receptor antagonist 2
  • HY-46286
    TTFB
    		Control
    TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel (ZAC) antagonist. TTFB inhibits Zn2+- and H+-induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
    TTFB
Cat. No. Product Name / Synonyms Application Reactivity