Catalog No.
Product Name
Application
Product Information
Citations
- Valnoctamide (MI-181) is discontinued (DEA controlled substance). It is a chiral constitutional isomer of valproic acid. It is a mild tranquilizer endowed with anticonvulsant properties, suggesting it may be an alternative treatment for epilepsy and bipolar disorder.
- Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm.
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GABAA receptor modulator
Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors. - 4-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system.
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Anxiolytic anticonvulsant
Etifoxine hydrochloride is potentiator of GABAA receptor function in cultured neurons. -
GABA-transaminase inhibitor
Vigabatrin is a structural analog of the inhibitory neurotransmitter ??-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase. -
anti-cancer agent
Ginsenoside Rc, isolated from Panax ginseng, may exert various activities including anti-cancer, anti-inflammatory, antiobesity, and anti-diabetic effects. -
GABA receptor agonist
Afloqualone, also known as HQ-495, is a centrally acting muscle relaxant. Afloqualone inhibits vestibular nystagmus probably due to both inhibition of selective polysynaptic transmission and enhancement of the effects of GABA and glycine in the lateral vestibular nucleus (LVN), and its GABA-enhancing effect is thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site. - L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5??-phosphate-dependent aminitransferase in E.
- (-)-Borneol is a bicyclic organic compound and a terpene derivative. The hydroxyl group in this compound is placed in an endo position. There are two different enantiomers of borneol. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
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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 antagonist
(-)-Securinine is an alkaloid originally isolated from S. suffructicosa. Securinine, is a specific GABA receptor antagonist and has been found to have significant in vivo CNS activity. -
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. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate (DHEA sulfate) functions as a GABA(A) receptor antagonist and a σ1 receptor agonist. This neurosteroid, primarily secreted by the adrenal gland, is capable of partially penetrating the blood-brain barrier. It inhibits GABA(A) receptor-mediated chloride influx while enhancing NMDA receptor activity via σ1 receptor interaction, displaying anti-inflammatory and antidepressant properties. DHEA sulfate is relevant for research in neuroprotection, depression, post-traumatic stress disorder (PTSD), and Alzheimer’s disease, and may serve as a biomarker for cardiovascular disease mortality due to its correlation with mortality rates. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate sodium (DHEA sulfate) primarily acts as a non-competitive GABA(A) receptor antagonist and σ1 receptor agonist. This neurosteroid, predominantly secreted by the adrenal gland, has demonstrated significant biological activities, including enhancing NMDA receptor function and exerting anti-inflammatory and antidepressant effects. DHEA sulfate sodium can penetrate the blood-brain barrier, making it valuable in research applications related to neuroprotection, neurite growth regulation, and neuropsychiatric disorders such as depression, post-traumatic stress disorder (PTSD), and Alzheimer's disease. Additionally, it may serve as a biomarker for cardiovascular disease mortality, with its levels inversely correlated with mortality rates. -
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. -
benzodiazepine receptor inverse agonist
Ro 19-4603 is a benzodiazepine receptor inverse agonist.
