GABA Receptor Modulator

GABA Receptor Modulators (43):

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 GABA_A?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 GABA_A receptor and an antagonist of GABA_C 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 GABA_A receptor α2/α3 subtype (K_is of 0.73 nM/2 nM) partial agonist and a α1 subtype (K_i 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 K_i 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-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-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-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 (GABA_A) 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 GABA_A receptor with an IC₅₀ of 17 nM and exerts anxiolytic effect.

HY-112788

ONO-8590580	Modulator	99.84%
ONO-8590580 is a GABA_A α5 negative allosteric modulator.

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-W009009

L-838417	Modulator	99.22%
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABA_A receptor and an antagonist at the α1, with binding K_i 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-123801

MIDD0301	Modulator	98.14%
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABA_A 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 GABA_A 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-19872

AZD-6280	Modulator	99.09%
AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.

HY-11048

NS11394	Modulator	99.77%
NS11394 is an orally active and unique subtype-selective GABA_A positive allosteric receptor (PAM), with a K_i of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABA_A-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.

HY-103503

CGP13501	Modulator
CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol.

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