1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor

GABA Receptor

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.

GABA Receptor Related Products (89):

Cat. No. Product Name Effect Purity
  • HY-N0219
    (+)-Bicuculline Antagonist 99.97%
    (+)-Bicuculline is a light-sensitive competitive antagonist of GABA-A receptor.
  • HY-101391
    Picrotoxin Antagonist >98.0%
    Picrotoxin is a noncompetitive antagonist of GABAA receptor.
  • HY-107994
    Aminooxyacetic acid hemihydrochloride Inhibitor >98.0%
    Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
  • HY-B0211
    Riluzole Inhibitor 99.83%
    Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-16716
    Basmisanil Inhibitor 99.49%
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  • HY-N0067
    γ-Aminobutyric acid Agonist
    γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors).
  • HY-B1671
    (+)-Kavain 99.98%
    (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
  • HY-W012123
    3,4,5-Trimethoxycinnamic acid Agonist 99.22%
    3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.
  • HY-15399
    Vigabatrin Inhibitor >98.0%
    Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase.
  • HY-B0007
    Baclofen Agonist 98.21%
    Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant.
  • HY-17354
    (R)-Baclofen Agonist >98.0%
    (R)-Baclofen(STX209) is a selective GABAB receptor agonist.
  • HY-16579A
    Etifoxine Activator 99.94%
    Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors.
  • HY-103531
    CGP52432 Antagonist 98.50%
    CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
  • HY-103040
    Zuranolone Agonist 99.93%
    Zuranolone (SAGE-217) is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  • HY-101107
    Allopregnanolone Modulator >98.0%
    Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor. Used to treat postpartum depression.
  • HY-B0211A
    Riluzole hydrochloride Inhibitor 99.94%
    Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-100228A
    SKF89976A hydrochloride Inhibitor 98.15%
    SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
  • HY-B0100
    Etomidate Agonist 99.33%
    Etomidate(R-16659) is a GABAA receptors agonist, which is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia.
  • HY-11048
    NS11394 Activator 99.84%
    NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
  • HY-B0009
    Flumazenil Antagonist 99.98%
    Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
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