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-124285
    ATPCA hydrochloride
    ATPCA hydrochloride is a selective radioactive substrate for BGT1 over GAT1/GAT3.
    ATPCA hydrochloride
  • HY-19371
    Lorediplon
    		Modulator 99.88%
    Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
    Lorediplon
  • HY-B0649S1
    Propofol-d18
    		Activator
    Propofol-d18 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission.
    Propofol-d<sub>18</sub>
  • HY-125296
    Fipronil sulfone
    		Inhibitor 99.85%
    Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
    Fipronil sulfone
  • HY-W005749
    (R)-4-Amino-3-hydroxybutyric acid
    		Agonist
    (R)-4-Amino-3-hydroxybutyric acid ((R)-GABOB) is a 4-aminobutyric acids (GABAB) agonist. (R)-4-Amino-3-hydroxybutyric acid is promising for research of nervous disorders.
    (R)-4-Amino-3-hydroxybutyric acid
  • HY-W012738
    DL-Pyroglutamic acid
    		Inhibitor 98.0%
    DL-Pyroglutamic acid (CAE) as an inactivator of hepatitis B surface, inactivates vaccinia virus, herpes simplex virus, and influenza virus except poliovirus. DL-Pyroglutamic acid is also a possible inhibitor of GABA transaminase, increases GABA amount with antiepileptic action.
    DL-Pyroglutamic acid
  • HY-101359
    TPMPA
    		Antagonist 98.1%
    TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells.
    TPMPA
  • HY-103505
    CL 218872
    		Modulator 99.25%
    CL 218872 is an orally active and selective ligand for the benzodiazepine receptor subtype BZ1. CL 218872 exhibits anxiolytic, sedative and anticonvulsant activities. CL 218872 can be used in researches of anxiety related disorders and epilepsy.
    CL 218872
  • HY-N0301
    Thiocolchicoside
    		Antagonist 99.54%
    Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
    Thiocolchicoside
  • HY-W050122
    S-(+)-GABOB
    S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor.
    S-(+)-GABOB
  • HY-B1229
    Isovaleramide
    		Modulator 98.0%
    Isovaleramide (3-Methylbutanamide) is an orally active anticonvulsant. Isovaleramide inhibits alcohol dehydrogenase (ADH) activity and regulates GABAergic system. Isovaleramide reduces acute kidney injury. Isovaleramide has antiepileptic, anxiolytic, sedative and hypnotic effects[1].
    Isovaleramide
  • HY-103524
    Valerenic acid
    		Activator 99.95%
    Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.
    Valerenic acid
  • HY-N2368A
    Arecaidine hydrochloride
    		Inhibitor 98.0%
    Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine hydrochloride
  • HY-U00315
    Gidazepam
    		Agonist 98.05%
    Gidazepam is an agonist of GABA receptor channels (GABA RCs).
    Gidazepam
  • HY-103534
    CI-966 hydrochloride
    		Inhibitor 99.60%
    CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.
    CI-966 hydrochloride
  • HY-N9483
    7-Keto-DHEA
    		Modulator 98.89%
    7-Keto-DHEA binds to GABA Receptor, and reduces the ethanol intake in rats. 7-Keto-DHEA exhibits potential in investigation of alcohol dependence disorders.
    7-Keto-DHEA
  • HY-W012735
    (+)-Nipecotic acid
    		≥98.0%
    (+)-Nipecotic acid ((+)-β-Homoproline) is a GABA transport inhibitor with potential antidepressant and anxiolytic activities. (+)-Nipecotic acid can increase the concentration of GABA in the synaptic cleft, thereby enhancing inhibitory neurotransmission. The research on (+)-Nipecotic acid provides a possible direction for the development of new inhibitory compounds for psychiatric diseases.
    (+)-Nipecotic acid
  • HY-103503
    CGP13501
    		Modulator 98.01%
    CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol.
    CGP13501
  • HY-19945
    DAA-1106
    		Agonist 99.93%
    DAA1106 is a peripheral benzodiazepine receptor (PBR) agonist that is permeable to the blood-brain barrier, but has no affinity for GABAA receptors.
    DAA-1106
  • HY-103511
    TCS1105
    		99.44%
    TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion.
    TCS1105
Cat. No. Product Name / Synonyms Application Reactivity