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-129927
    Thiomuscimol
    		Agonist
    Thiomuscimol is a GABAA receptor agonist (IC50=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
    Thiomuscimol
  • 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-101411R
    4-Acetamidobutanoic acid (Standard)
    		Agonist
    Josamycin propionate (Standard) is the analytical standard of Josamycin propionate. This product is intended for research and analytical applications. Josamycin propionate is classified as a macrolide antibiotic.
    4-Acetamidobutanoic acid (Standard)
  • 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-B0135S
    Furosemide-d5
    		Antagonist 99.57%
    Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. 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[2].
    Furosemide-d<sub>5</sub>
  • 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-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-D1704
    Bodipy TMR-X muscimol
    		Agonist
    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-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 methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (+)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca2+-activated K+ channels in various types of neurons.
    (+)-Bicuculline methochloride
Cat. No. Product Name / Synonyms Application Reactivity