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-170771
    α5-GABAA receptor modulator 1
    		Modulator
    α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABAA receptor, suitable for research into central nervous system (CNS) disorders.
    α5-GABAA receptor modulator 1
  • HY-107482A
    Picamilon sodium
    		Agonist
    Picamilon sodium is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon sodium improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.
    Picamilon sodium
  • HY-161784
    GABAA receptor modulator-5
    		Modulator
    GABAA receptor modulator-5 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC50 of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression.
    GABAA receptor modulator-5
  • HY-100783B
    Bicuculline methobromide
    		Antagonist
    Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders.
    Bicuculline methobromide
  • HY-113320R
    Etiocholanolone (Standard)
    		Modulator
    Cimbuterol (Standard) is the analytical standard of Cimbuterol. This product is intended for research and analytical applications. Cimbuterol is a β-adrenergic receptor agonist.
    Etiocholanolone (Standard)
  • HY-134912
    CMPPE
    		Modulator
    CMPPE is a GABAB receptor positive allosteric modulator (PAM) that inhibits alcohol self-administration and reinstatement behavior in rats.
    CMPPE
  • HY-130670
    CGP 54626A free base
    		Modulator
    CGP 54626A (free base) is a GABAB receptor modulator, which is essential in the central and peripheral nervous systems. It is used as a tool to identify and characterize GABAB receptor agonists and antagonists, which will aid in the development of drugs targeting diseases related to these systems. This discovery involves purified GABAB receptors, receptor proteins and their encoding nucleic acids, facilitating the study of new members of the GABAB receptor family through DNA cloning technology and sequence-derived probes.
    CGP 54626A free base
  • HY-124463
    Epiallopregnanolone
    		Antagonist
    Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer.
    Epiallopregnanolone
  • HY-147657
    GABAA receptor modulator-2
    		Modulator
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety.
    GABAA receptor modulator-2
  • HY-155498
    TETS-4-Methylaniline
    		Inhibitor
    TETS-4-Methylaniline (compound 2k) is a hapten. TETS-4-Methylaniline conjugates to the carrier protein via using either diazotization or glutaraldehyde methods.
    TETS-4-Methylaniline
  • HY-103526
    DPNI-GABA
    		Inhibitor
    DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC50 value of 0.5 mM.
    DPNI-GABA
  • HY-168986
    Moxetomidate
    		Agonist
    Moxetomidate is a GABAA receptor agonist with hypnotic effect.
    Moxetomidate
  • HY-B1594R
    Carbromal (Standard)
    		Agonist
    Carbromal (Standard) is the analytical standard of Carbromal. This product is intended for research and analytical applications. Carbromal (Adalin; Adisomnol) is a sedative with centrally depressant effects.
    Carbromal (Standard)
  • HY-103495
    17-PA
    		Antagonist
    17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABAA receptors.
    17-PA
  • HY-W007686R
    Imidazoleacetic acid hydrochloride (Standard)
    Imidazoleacetic acid (hydrochloride) (Standard) is the analytical standard of Imidazoleacetic acid (hydrochloride). This product is intended for research and analytical applications. Imidazoleacetic acid hydrochloride is a γ-aminobutyric acid receptor agonist. Imidazoleacetic acid hydrochloride inhibits GABA-T in a non-competitive manner, with a Ki value of 0.34 mM. Imidazoleacetic acid hydrochloride increases total free GABA in brain[1][2][3].
    Imidazoleacetic acid hydrochloride (Standard)
  • HY-110234R
    Topiramate D12 (Standard)
    		Activator
    Topiramate D12 (Standard) is the analytical standard of Topiramate D12. This product is intended for research and analytical applications. Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
    Topiramate D12 (Standard)
  • HY-106547
    Rilmazafone
    Rilmazafone is a benzodiazepine (omega) ligand and an orally active sleep inducer.
    Rilmazafone
  • HY-169193
    Azocarnil
    		Agonist
    Azocarnil is a GABAergic agonist-potentiator. Azocarnil can be used in neurological research.
    Azocarnil
  • HY-123840
    MRK-623
    		Agonist
    MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect.
    MRK-623
  • HY-123249
    HZ166
    		Agonist
    HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects. HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HZ166
Cat. No. Product Name / Synonyms Application Reactivity