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-156061
    NAP-1
    		Agonist
    NAP-1 is a compound with agent that can suppress or relieve pain. effects. NAP-1 enhances the inhibitory current by binding to a specific site of GABAaR, resulting in a narcotic effect. NAP-1 can be used in research to develop clinical agent that can suppress or relieve pain.
    NAP-1
  • HY-175251
    GABAA receptor modulator-9
    		Modulator
    GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype GABAA that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC50: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC50s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE).
    GABAA receptor modulator-9
  • HY-182041
    Insecticidal agent 31
    		Inhibitor
    Insecticidal agent 31 is an insecticide targeting the γ-aminobutyric acid receptor (GABAR). Insecticidal agent 31 exhibits insecticidal activity against Plutella xylostella, Spodoptera frugiperda and Spodoptera exigua. Insecticidal agent 31 can serve as a lead compound for the design and synthesis of novel isoxazole-based insecticides.
    Insecticidal agent 31
  • HY-N3478
    Isohyenanchin
    		Antagonist
    Isohyenanchin (Hydroxycoriatin) is an RDLac homo-oligomers antagonist. Isohyenanchin also is a weak antagonist of ionotropic GABA receptors.
    Isohyenanchin
  • HY-167650
    Fletazepam
    		Agonist
    Fletazepam is a benzodiazepine derivative with sedative, anxiolytic and muscle relaxant effects. Fletazepam can be utilized in neurological research.
    Fletazepam
  • HY-11058
    BHF177
    		Modulator
    BHF177 is a positive modulator of GABAB receptors that can block the interaction between nicotine and the brain's dopamine system, thereby reducing the addictive properties of nicotine. BHF177 is expected to be used in research related to smoking cessation.
    BHF177
  • HY-162757
    Anticonvulsant agent 5
    		Modulator
    Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable.
    Anticonvulsant agent 5
  • HY-115854
    Ro 15-1310
    		Inhibitor
    Ro 15-1310 is an imidazobenzodiazepine that exhibits high affinity and selectivity for alpha 5-containing GABAA receptors. Ro 15-1310 is promising for research of convulsions.
    Ro 15-1310
  • HY-160978
    Timelotem
    		Agonist
    Timelotem (KC-7507 free base) is a representative of a class of 1, 2-cyclo1, 4-benzodiazepines. Timelotem shows significant antipsychotic properties. Timelotem produces sedative, anti-anxiety and anti-convulsant effects by enhancing the action of the neurotransmitter gamma-aminobutyric acid (GABA). Timelotem can be used in studies of schizophrenia and other mental disorders.
    Timelotem
  • HY-159624
    KK-92A
    		Modulator
    KK-92A, a blood-brain barrier penetrated GABAB positive allosteric modulator (PAM), suppresses alcohol self-administration and cue-induced reinstatement of alcohol seeking in rats.
    KK-92A
  • HY-P992360
    GT-002
    		Modulator
    GT-002 is a partial positive allosteric modulator targeting the α3 subtype of GABAA receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency.
    GT-002
  • HY-B0007A
    (S)-Baclofen hydrochloride
    		Agonist
    (S)-Baclofen hydrochloride is a GABAB receptor agonist that crosses the blood-brain barrier and is orally active, with IC50 values ​​of 1.77 μM for GABAB and 1564 μM for GABAA. (S)-Baclofen hydrochloride can be used in research on muscle disorders such as spasticity.
    (S)-Baclofen hydrochloride
  • HY-100842A
    (S)-3C4HPG
    		Antagonist
    (S)-3C4HPG is a metabotropic glutamate receptor antagonist, demonstrating significant potential in modulating neuronal excitability and influencing synaptic transmission.
    (S)-3C4HPG
  • HY-108035
    (-)-JM-1232
    (-)-JM-1232 (MR04A3) targets GABA A receptors and exerts its analgesic effects by binding to the benzodiazepine binding site of GABA A receptors. (-)-JM-1232 demonstrates potent analgesic effects in mice against acute thermal stimuli, mechanically induced pain, and visceral pain, with CI50 values of 2.96, 3.06, and 2.27 mg/kg, respectively. (-)-JM-1232 can be used in research related to pain and analgesia.
    (-)-JM-1232
  • HY-145257
    GABAA receptor agent 5
    		Antagonist
    GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an Ki of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability.
    GABAA receptor agent 5
  • HY-W070739
    GABAA receptor modulator-12
    		Modulator
    GABAA receptor modulator-12 (Compound 5) is a GABAA receptor modulator. GABAA receptor modulator-12 inhibits anesthetic-induced desensitization of GABAA α3β3γ2 receptors with an IC50 of 0.2 μM. GABAA receptor modulator-12 can be used in the research of central nervous system disorders.
    GABAA receptor modulator-12
  • HY-W742300
    Pipazethate hydrochloride
    		Antagonist
    Pipazethate (SKF 70230A; SQ 15874) hydrochloride is a potent GABA antagonist. Pipazethate hydrochloride shows antitussive activity and can be used in research in cough suppressant .
    Pipazethate hydrochloride
  • HY-116944
    Ro 17-1812
    		Agonist
    Ro 17-1812 is a benzodiazepine receptor partial agonist with anticonvulsant effect.
    Ro 17-1812
  • HY-100915
    SKF 97541
    		Agonist
    SKF 97541 (CGP 35024) is a potent and selective GABAB agonist that can induce hyperpotential. SKF 97541 has antiepileptic activity.
    SKF 97541
  • HY-167702
    (Rac)-Acetoxyvalerenic acid
    		Modulator
    (Rac)-Acetoxyvalerenic acid is a derivative of valerenic acid that acts as a GABA (A) receptor modulator, potentially providing sedative and sleep-enhancing effects. (Rac)-Acetoxyvalerenic acid exhibits slower permeability across the blood-brain barrier compared to diazepam, indicating that its transport may rely on an unidentified pathway rather than transcellular passive diffusion.
    (Rac)-Acetoxyvalerenic acid
Cat. No. Product Name / Synonyms Application Reactivity