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)
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GABA transport inhibitor
(S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug. -
BzR agonist
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively. -
GABAA receptor modulator
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, -
GABA(A) receptor agonist
Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure. -
GABA uptake inhibitor
Guvacine hydrochloride inhibits GABA uptake (IC50 values are 14, 58, 119 and 1870 uM for hGABA T-1, rGABA T-2, hGABA T-3 and hBGT-1 respectively). -
GABAB receptors antagonist
2-Hydroxysaclofen is a potent and selective antagonist at GABAB receptors. -
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. - Ethyl dirazepate is a drug which is a benzodiazepine derivative. It has anxiolytic and hypnotic and possibly other characteristic benzodiazepine properties.
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GABA antagonist
Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide. -
benzodiazepine receptor antagonist
Ro 15-1788 is a benzodiazepine receptor antagonist. - 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 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.