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

Related Products

PDF 3.03 MB

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-178482
    HDZI 2,4OH
    		Inhibitor
    HDZI 2,4OH exerts significant anti anxiety activity through GABA receptors. HDZI 2,4OH can penetrate the blood-brain barrier. HDZI 2,4OH exhibits low toxicity in zebrafish. HDZI 2,4OH can be used for research on neurological disorders such as anxiety disorders.
    HDZI 2,4OH
  • HY-118259
    L-663581
    		Agonist
    L-663581 (FG-8205) is an agonist of benzodiazepine receptor, acting as a partial agonist at GABA A receptor.
    L-663581
  • HY-W634748
    Desalkylgidazepam
    		Agonist
    Desalkylgidazepam is a benzodiazepine compound and Gidazepam (HY-U00315) metabolite. Desalkylgidazepam can activate GABA A receptor and translocator protein (TSPO).
    Desalkylgidazepam
  • HY-P5857
    MmTx2 toxin
    		Modulator
    MmTx2 toxin is a GABAA receptor modulator that enhances GABAA receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain.
    MmTx2 toxin
  • HY-180372
    CSP-2503
    CSP-2503 is a potent and selective 5-HT1A receptor agonist , with an EC50 of 0.15 μM and a Ki of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (Ki > 1000 nM), 5-HT4 receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.
    CSP-2503
  • HY-170498
    GABA-A Receptor Ligand-1
    		Ligand
    GABA-A Receptor Ligand-1 (Compound 4) is a ligand for GABA-A receptor with a pKi of 7.27. GABA-A Receptor Ligand-1 reduces mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration. GABA-A Receptor Ligand-1 exhibits neuroprotective efficacy in rats ischemic stroke models.
    GABA-A Receptor Ligand-1
  • HY-180087
    GABA-AT-IN-2
    		Inhibitor
    GABA-AT-IN-2 (compound 11g) is a GABA aminotransferase (GABA-AT) inhibitor with an IC50 of 19.8 μM. GABA-AT-IN-2 demonstrates notable antianxiety effects in mice. GABA-AT-IN-2 can be used for anxiety-related neurotic disorders research.
    GABA-AT-IN-2
  • HY-118207
    LU-32-176B
    		Inhibitor
    LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively.
    LU-32-176B
  • HY-105481
    CGS-17867A hydrochloride
    		Ligand
    CGS-17867A hydrochloride is a benzodiazepine receptor ligand. CGS-17867A hydrochloride has a weak sedative effect and can increase palatable food intake.
    CGS-17867A hydrochloride
  • HY-P11382
    Octadecaneuropeptide
    Octadecaneuropeptide is an 18-residue peptide. Octadecaneuropeptide can be derived from Diazepam binding inhibitor. Octadecaneuropeptide includes a specific ligand for the gamma-aminobutyric acid receptor regulatory site occupied by beta-carbolines. Octadecaneuropeptide elicits a dose-related facilitation of the punishment- elicited suppression of drinking.
    Octadecaneuropeptide
  • HY-116859
    Ro 14-7437
    		Antagonist
    Ro 14-7437 is a potent and selective potentiating antagonist of Midazolam.
    Ro 14-7437
  • HY-116457
    Propanidid
    		Agonist 98.19%
    Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA) receptor agonist and a short-acting non-barbiturate general agent that can suppress or relieve pain. Propanidid can decrease the arterial pressure.
    Propanidid
  • HY-175670
    GABAA receptor modulator-10
    		Agonist
    GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy.
    GABAA receptor modulator-10
  • HY-117256
    Gabazine free base
    		Antagonist
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of 0.2 μM for GABA receptor.
    Gabazine free base
  • HY-185007
    LI-633
    		Agonist
    LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a Ki of 21 nM. LI-633 produces robust potentiation of GABA-induced inward current, with EC50 values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 potentiates muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons with an EC50 of 70.4 nM. LI-633 can be used for the study of visceral pain.
    LI-633
  • HY-10061A
    Lesogaberan napadisylate
    		Agonist
    Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan napadisylate
  • HY-159826
    Brexanolone caprilcerbate
    		Agonist
    Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator.
    Brexanolone caprilcerbate
  • HY-146280
    mGAT3/4-IN-1
    		Inhibitor
    mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice.
    mGAT3/4-IN-1
  • HY-169432
    TET-13
    		Modulator
    TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively).
    TET-13
  • HY-13694R
    Methionine (Standard)
    		Activator
    Methionine (Standard) is the analytical standard of Methionine. This product is intended for research and analytical applications. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity