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-103522
    AA29504
    		Inhibitor
    AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(HY-L120) receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases .
    AA29504
  • HY-B0007B
    (S)-Baclofen
    		Agonist
    (S)-Baclofen 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 can be used in research on muscle disorders such as spasticity.
    (S)-Baclofen
  • HY-116152A
    (S)-Cipepofol
    (S)-Cipepofol is the isomer of Cipepofol (HY-116152).Cipepofol (HSK3486) is a sleep-promoting active molecule and a gamma-aminobutyric acid (GABA) receptor enhancer.
    (S)-Cipepofol
  • HY-113320S1
    Etiocholanolone-d2
    		Modulator
    Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form.
    Etiocholanolone-d<sub>2</sub>
  • HY-115857
    SH-053-S-CH3-2'F
    SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs.
    SH-053-S-CH3-2'F
  • HY-149399
    GABA-IN-1
    		Inhibitor
    GABA-IN-1 (Compound 6) is a GABA inhibitor. GABA-IN-1 has larvicidal activity and insecticidal effect, with mortality rates of 93% at 50 mg/L.
    GABA-IN-1
  • HY-167973
    GABA-palmitamide
    GABA-palmitamide is a GABA-responsive compound. GABA-palmitamide exhibits a dose-dependent bidirectional regulatory effect on the stereotyped behavior induced by Apomorphine (HY-12723): high doses inhibit motor behavior, while low doses enhance stereotyped behaviors in the oral cavity. GABA-palmitamide can be used in research on behavior regulation.
    GABA-palmitamide
  • HY-105059A
    Denzimol hydrochloride
    Denzimol hydrochloride is an orally active anticonvulsant agent.
    Denzimol hydrochloride
  • HY-W709349S
    Flupirtine-d6 hydrochloride
    		Activator
    Flupirtine-d6 (D 9998-d6) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
    Flupirtine-d<sub>6</sub> hydrochloride
  • HY-129907
    2-AEMP
    2-AEMP (2-Aminoethyl methylphosphonate) is an anti-GABA(A)-ρ1 receptor compound with antagonist activity. 2-AEMP exhibits competitive inhibition compared to TPMPA with an IC(50) value of 18 μM, compared to 7 μM for TPMPA. The release rate of inhibition at termination of 2-AEMP is significantly higher than that of TPMPA. The preincubation time required for the onset of inhibition of 2-AEMP is much shorter than that of TPMPA. Some analogs of 2-AEMP, especially those with benzyl or n-butyl substituents, show lower potency in terms of biological activity.
    2-AEMP
  • HY-W739289
    Californidine perchlorate
    		Modulator
    Californidine perchlorate is an orally active γ-aminobutyric acid (GABA) receptor and serotonin receptor modulator. Californidine perchlorate enhances GABA-mediated chloride influx and inhibits cytochrome P450 enzymes. Californidine perchlorate is promising for research of anxiety.
    Californidine perchlorate
  • HY-182548
    BTS 72664
    BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABAA receptor (GABAA receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na+ channels (Ki = 350 μM) and NMDA receptors (NMDA receptor) (IC50 = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine.
    BTS 72664
  • HY-W778008
    Rac-Vigabatrin-13C,d2
    Rac-Vigabatrin-13C,d2 (Major) is the deuterium and 13C labeled Vigabatrin (HY-15399). Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
    Rac-Vigabatrin-<sup>13</sup>C,d<sub>2</sub>
  • HY-151950
    Antidepressant agent 3
    Antidepressant agent 3 is an orally active antidepressant agent. Antidepressant agent 3 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 3
  • HY-W700174
    3-(4-Chlorophenyl)-4-hydroxybutyric acid sodium
    3-(4-Chlorophenyl)-4-hydroxybutyric acid sodium is an inactive metabolite of the GABAB receptor agonist Baclofen (HY-B0007).
    3-(4-Chlorophenyl)-4-hydroxybutyric acid sodium
  • HY-101643
    RP-60503
    RP-60503 is an orally active anxiolytic cyclopyrrolone derivative with low sedative potential. RP-60503 binds to the gamma-aminobutyric acidA (GABA)/benzodiazepine receptor with a Ki value of 1.16 nM. RP-60503 can be used for the research of neurological disease.
    RP-60503
  • HY-123222
    CGP 56999
    		Antagonist
    CGP 56999 is a potent antagonist GABA(B) receptor, with the IC50 of 0.002 μM. CGP 56999 increased the levels of BDNF mRNA in the brain in vivo and in vitro.
    CGP 56999
  • HY-145256
    GABAA receptor agent 4
    		Antagonist
    GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential.
    GABAA receptor agent 4
  • HY-W740139
    4-Hydroxy midazolam methanoate-d5
    4-Hydroxy midazolam methanoate-d5 is the deuterium labeled 4-Hydroxymidazolam (HY-100050). 4-Hydroxymidazolam is a major metabolite of Midazolam. Midazolam is a potent benzodiazepine with anxiolytic properties.
    4-Hydroxy midazolam methanoate-d<sub>5</sub>
  • HY-109156
    Pregabalin arenacarbil
    		Activator
    Pregabalin arenacarbil is a proagent of Pregabalin.Pregabalin is an analog of gamma-aminobutyric acid (GABA) for the research of post herpetic neuralgia, peripheral diabetic neuropathy,fibromyalgia and epilepsy.
    Pregabalin arenacarbil
Cat. No. Product Name / Synonyms Application Reactivity