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-177099
    Lorotomidate
    		Agonist
    Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED50: i.v., 2 mg/kg in KM mice; LD50: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.
    Lorotomidate
  • HY-119105
    LY81067
    LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites.
    LY81067
  • HY-103513
    GABAA receptor agent 2
    		Modulator
    GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
    GABAA receptor agent 2
  • HY-19438
    Divaplon
    		Agonist
    Divaplon is a GABA receptor agonist with the EC50 values of 31 and 2 nM for α3β2γ2 and α5β2γ2, respectively. Divaplon shows anxiolytic activity.
    Divaplon
  • HY-146100
    GABAA receptor agent 8
    		Inhibitor
    GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy.
    GABAA receptor agent 8
  • HY-123240
    CI-966
    		Inhibitor
    CI-966 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 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities.
    CI-966
  • HY-111298
    TG 41
    		Modulator
    TG 41 is positive modulator of GABAA receptor. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes.
    TG 41
  • 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-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-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-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
Cat. No. Product Name / Synonyms Application Reactivity