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Catalog No.
Product Name
Application
Product Information
Product Citation
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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. -
GABA receptor agonist
Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction. -
GABAA α5 receptor agonist
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA?α1β3γ2, GABAA?α2β3γ2, GABAA?α3β3γ2, and GABAA?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS. -
Benzodiazepine receptor agonist
Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity. -
GABAA antagonist
(+)-Bicuculline is a classical GABAA antagonist.- Maryam Adenike Salaudeen, .et al. , J Pharmacy and Drug Innovations, 2022, 3(4)
- Phenazepam is a benzodiazepine agonist of the ??-aminobutyric acid A (GABAA)-benzodiazepine receptor chloride channel complex.
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GABAA receptor modulator
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, -
GABAA receptor agonist
AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models. -
GABAA agonist
Bretazenil, a benzodiazepine receptor partial agonist, as an adjunct in the prophylactic treatment of OP poisoning. -
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 reuptake inhibitor
Tiagabine is an anti-convulsive medication. The medication is also utilized in the treatment of panic disorder, as are a few other anticonvulsants. -
GABA receptor agonist
Piperazine is an organic compound that consists of a six-membered ring containing two nitrogen atoms at opposite positions in the ring. -
GABAB receptor agonist
(R)-Baclofen(STX209) is a selective GABAB receptor agonist. -
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 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.
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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. - Propofol is a hypnotic alkylphenol derivative. Propofol is a General Anesthetic. Propofol is a short-acting medication that results in a decreased level of consciousness and lack of memory for events. Formulated for intravenous induction of sedation and hypnosis during anesthesia, propofol facilitates inhibitory neurotransmission mediated by gamma-aminobutyric acid (GABA).
- 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 agonist
Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. - 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.
