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-106917
    Lirequinil
    		Agonist
    Lirequinil (Ro 41-3696) is an orally active partial agonist of the benzodiazepine (BDZ) receptor. Lirequinil has the effect of promoting sleep.
    Lirequinil
  • HY-N0067S2
    γ-Aminobutyric acid-4,4-d2
    		Agonist
    γ-Aminobutyric acid-4,4-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-4,4-d<sub>2</sub>
  • HY-N0659R
    Jujuboside A (Standard)
    		Agonist
    Jujuboside A (Standard) is the analytical standard of Jujuboside A. This product is intended for research and analytical applications. Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, a Chinese herbal medicine used to treat insomnia and anxiety.
    Jujuboside A (Standard)
  • HY-147735
    GABAA receptor agonist 1
    		Agonist
    GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression.
    GABAA receptor agonist 1
  • HY-103496
    U-90042
    		Agonist
    U-90042 is a gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with Ki values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent.
    U-90042
  • HY-105272A
    Loreclezole hydrochloride
    		Agonist
    Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
    Loreclezole hydrochloride
  • HY-113726
    Nerisopam
    		Agonist
    Nerisopam is an orally active gamma-aminobutyric acid (GABA) receptor agonist. Nerisopam is an anxiolytic and antipsychotic homophthalazine. Nerisopam induces rapid, intense expression of Fos-like immunoreactivity in the rostral, dorsomedial and lateral parts of the striatum in the rat.
    Nerisopam
  • HY-19266
    RO-488684
    		Agonist
    RO-488684 is a benzodiazepine receptor agonist. RO-488684 can be used for research on sleep and conscious sedation.
    RO-488684
  • HY-B0007R
    Baclofen (Standard)
    		Agonist
    Baclofen (Standard) is the analytical standard of Baclofen. This product is intended for research and analytical applications. 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 (Standard)
  • HY-105518
    Terbequinil
    		Agonist
    Terbequinil (SR-25776) is a potent orally active Gamma-aminobutyric acid A (GABAA) receptor inverse agonist. Terbequinil can be used for research on nervous system diseases.
    Terbequinil
  • HY-103498A
    Org 20599 methanesulfonate
    		Agonist
    Org20599 methanesulfonate is a direct agonist of the GABAA receptor with an EC50 of 1.1 μM. Org20599 methanesulfonate can be used in the research of neurological disorders.
    Org 20599 methanesulfonate
  • HY-123489S
    3α,21-Dihydroxy-5α-pregnan-20-one-d3
    		Agonist
    3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
    3α,21-Dihydroxy-5α-pregnan-20-one-d<sub>3</sub>
  • HY-115763
    3-Aminopropylphosphinic acid
    		Agonist
    3-Aminopropylphosphinic acid (3-APPA) is a phosphonic analog of GABA. 3-Aminopropylphosphinic acid is a potent, selective GABAB receptor agonist.
    3-Aminopropylphosphinic acid
  • HY-B2177R
    Apronal (Standard)
    		Agonist
    Apronal (Standard) is the analytical standard of Apronal. This product is intended for research and analytical applications. Apronal (Allylisopropylacetylurea, Apronalide) can bu used for the research of neuropsychiatry disorders.
    Apronal (Standard)
  • HY-170903
    GABAA receptor modulator-3
    		Agonist
    GABAA receptor modulator-3 (compound 3b) is a positive allosteric modulator (PAM). GABAA receptor modulator-3 inhibits α1β3γ2 GABAAR at peak and steady state currents with IC50s of 671 and 64 μM, respectively.
    GABAA receptor modulator-3
  • 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity