2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. GABA Receptor
  5. GABA Receptor Modulator

GABA Receptor Modulator

GABA Receptor Modulators (44):

Cat. No. Product Name Effect Purity
  • HY-N0662
    Amentoflavone
    		Modulator 99.81%
    Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.
  • HY-113320
    Etiocholanolone
    		Modulator 99.31%
    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.
  • HY-B0799
    Dihydroergotoxine mesylate
    		Modulator 99.88%
    Dihydroergotoxine mesylate is a series of alkaloid salt mixtures with high binding activity to GABAA receptors.
  • HY-10233
    Gaboxadol hydrochloride
    		Modulator 99.85%
    Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.
  • HY-19505
    TPA-023B
    		Modulator 98.58%
    TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.
  • HY-153584
    MRK-898
    		Modulator 99.48%
    MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s).
  • HY-19371
    Lorediplon
    		Modulator 99.78%
    Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
  • HY-121618
    α-Thujone
    		Modulator 98.07%
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
  • HY-N0549
    (-)-α-Pinene
    		Modulator 98.30%
    (-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
  • HY-100936
    Etazolate hydrochloride
    		Modulator 98.00%
    Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
  • HY-W013150
    Alpidem
    		Modulator 99.49%
    Alpidem selectively binds to α1β2γ2 subunit-containing GABAA receptor with an IC50 of 17 nM and exerts anxiolytic effect.
  • HY-112788
    ONO-8590580
    		Modulator 99.84%
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
  • HY-19872
    AZD-6280
    		Modulator 99.09%
    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
  • HY-103502
    CGP7930
    		Modulator ≥99.0%
    CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons.
  • HY-113320S
    Etiocholanolone-d5
    		Modulator 99.20%
    Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].
  • HY-123801
    MIDD0301
    		Modulator 98.14%
    MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases.
  • HY-B1803A
    Tracazolate hydrochloride
    		Modulator 99.03%
    Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
  • HY-W009009
    L-838417
    		Modulator 99.22%
    L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
  • HY-11048
    NS11394
    		Modulator 99.77%
    NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
  • HY-103501
    SB-205384
    		Modulator
    SB-205384 is a GABAA receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist.