Catalog No.
Product Name
Application
Product Information
Citations
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Chloride Channel/GABA Receptor blocker
Picrotoxinin negatively modulate the action of GABA on GABAA receptors. -
GABA receptor agonist
Tramiprosate, also known as homotaurine, is a gamma-Aminobutyric acid (GABA) receptor agonist and a glycosaminoglycan mimetic used in the treatment of Alzheimer's disease. -
GABA agonist
Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing It acts at spinal and supraspinal sites, reducing excitatory transmission. -
GABA Receptor Modulator
α-Thujone is a monoterpene that acts as a reversible modulator of the GABA type A receptor, with an IC50 of 21 μM for inhibiting GABA-induced currents. This compound demonstrates significant anti-tumor activity by inducing reactive oxygen species (ROS) accumulation, as well as promoting cell apoptosis and autophagy. Additionally, α-Thujone exhibits antinociceptive, insecticidal, and anthelmintic properties, while being capable of crossing the blood-brain barrier, making it valuable for various biological research applications. -
GABAA Receptor Agonist
Cipepofol is a positive allosteric modulator and direct agonist of the GABAA receptor. This compound demonstrates significant central nervous system inhibition and promotes sleep, offering potential applications in anesthesia and sleep research. Additionally, Cipepofol activates the Sirtuin1 (Sirt1)/Nrf2 pathway, providing cardioprotective effects against isoproterenol-induced myocardial infarction by reducing oxidative stress, inflammatory responses, and cardiomyocyte apoptosis. -
GABAB Receptor Negative Allosteric Modulator
(E/Z)-CLH304a is a negative allosteric modulator of the GABAB receptor, consisting of a mixture of (E)-CLH304a and (Z)-CLH304a. This compound selectively inhibits the GABAB receptor and noncompetitively modulates its activity. Research has demonstrated that (E)-CLH304a is effective in blocking Baclofen-induced ERK1/2 phosphorylation in HEK293 cells that overexpress GABAB receptors, making it a valuable tool for studies investigating GABAB receptor signaling pathways and their implications in neurological disorders. - Chlormezanone (Trancopal), a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
Benzodiazepine antagonist
Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in humans. - Furosemide is a non-competitive antagonist at GABAA receptors with ~ 100-fold greater selectivity for α6-containing receptors than α1-containing receptors.
- Nefiracetam is cognitive enhancer. It activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems.
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GABA uptake inhibitor
SKF 89976A hydrochloride is a potent inhibitor of GABA uptake with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. -
partial benzodiazepine receptor agonist
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity. -
GABAA receptors agonist
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a selective agonist at GABAA receptors that contain α4-δ subunits, and has anxiolytic and sedative effects. -
Benzodiazepine inverse agonist
DMCM (hydrochloride) is Benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity. -
GABAB receptor positive allosteric modulator
SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator. -
GABA-A modulator
Imidazenil is a GABA-A modulator that blocks the sedative effects without lowering the convulsion threshold. -
nervoussystem toxicant
Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. - 4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyric acid (GABA) derivative.
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GABA receptor agonist
Isoguvacine hydrochloride is a GABA receptor agonist. - Piperazine Citrate is an organic compound that consists of a six-membered ring, containting two nitrogen atoms at opposite positions in the ring; first introduced in 1953 as an Anthelmintic.
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chemoprotective agent
Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation. -
GABAAα5 modulator
Basmisanil is a highly selective GABAAα5 negative allosteric modulator. -
GABAA receptor partial agonist
CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity. -
BDZ receptor agonist
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for ?CGABA and +GABA respectively. -
GABAA receptor agonist
Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. - Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
- Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
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GABAA α5 inverse agonist
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively). - Rilmazafone is a water-soluble benzodiazepine prodrug that acts as a sedative and hypnotic neuropsychiatric agent.
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benzodiazepine receptor antagonist
Sarmazenil is a benzodiazepine receptor antagonist. -
benzodiazepine receptor inverse agonist
Ro 19-4603 is a benzodiazepine receptor inverse agonist. -
GABA receptor antagonist
Gabazine free base is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites. -
pyrazolopyridine anxiolytic
Tracazolate is a pyrazolopyridine anxiolytic known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases.
