GABA Receptors

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  1. HIV-1 production Inhibitor

    Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.
  2. Dihydropyrimidinase Inhibitor

    Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects.
  3. 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.
  4. Furosemide is a non-competitive antagonist at GABAA receptors with ~ 100-fold greater selectivity for α6-containing receptors than α1-containing receptors.
  5. Gabapentin (Neurontin) is a pharmaceutical agent, specifically a GABA analogue.
  6. Gabapentin Hydrochloride is a GABA analogue.
  7. Nefiracetam is cognitive enhancer. It activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems.
  8. Primidone is an anticonvulsant. Potentiates GABAA receptor function.
  9. 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.
  10. 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.
  11. 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.
  12. Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
  13. Benzodiazepine receptor agonist

    Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
  14. GABAA antagonist

    (+)-Bicuculline is a classical GABAA antagonist.
  15. GABAA receptor antagonist

    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
  16. 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.
  17. partial agonist of GABA(A) receptor

    RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
  18. GABA reuptake inhibitor

    Tiagabine is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
  19. Benzodiazepine receptor/GABAA receptor agonist

    U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.
  20. 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.
  21. GABAA receptor modulator

    Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator,
  22. GABA(A) receptor agonist

    Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure.
  23. 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).
  24. benzodiazepine1 (BZ1) receptor agonist

    SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.
  25. GABAB receptors antagonist

    2-Hydroxysaclofen is a potent and selective antagonist at GABAB receptors.
  26. GABAA receptor agonist

    AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
  27. GABAA receptor modulator

    Indiplon is a pyrazolopyrimidine that acts as a high-affinity positive allosteric modulator of the GABAA receptor, potentiating GABA-activated chloride currents in a dose-dependent and reversible manner.
  28. GABAA agonist

    Bretazenil, a benzodiazepine receptor partial agonist, as an adjunct in the prophylactic treatment of OP poisoning.
  29. Ethyl dirazepate is a drug which is a benzodiazepine derivative. It has anxiolytic and hypnotic and possibly other characteristic benzodiazepine properties.
  30. GABA antagonist

    Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide.
  31. Oxiracetam is a cyclic derivative of gamma-aminobutyric acid (GABA).
  32. Benzodiazepine agonist

    a5IA is a nootropic drug invented in 2004 by a team working for Merck, Sharp and Dohme, which acts as a subtype-selective inverse agonist at the benzodiazepine binding site on the GABAA receptor.
  33. benzodiazepine receptor antagonist

    Ro 15-1788 is a benzodiazepine receptor antagonist.
  34. 4-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system.
  35. Anxiolytic anticonvulsant

    Etifoxine is potentiator of GABAA receptor function in cultured neurons.
  36. Anxiolytic anticonvulsant

    Etifoxine hydrochloride is potentiator of GABAA receptor function in cultured neurons.
  37. 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.
  38. anti-cancer agent

    Ginsenoside Rc, isolated from Panax ginseng, may exert various activities including anti-cancer, anti-inflammatory, antiobesity, and anti-diabetic effects.
  39. GABA(A) modulator

    CTP354 a novel deuterated subtype-selective GABA(A) modulator.
  40. 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.
  41. 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.
  42. GABAA receptor ligand

    U-93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.
  43. GABAB receptor agonist

    (R)-Baclofen(STX209) is a selective GABAB receptor agonist.
  44. 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.
  45. GABA receptor agonist

    Bamaluzole is a GABA receptor agonist.
  46. GABA-A receptor antagonist

    Cgp 52432 is a GABA-A receptor antagonist.
  47. 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.
  48. L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5??-phosphate-dependent aminitransferase in E.
  49. Chloride Channel/GABA Receptor blocker

    Picrotoxinin negatively modulate the action of GABA on GABAA receptors.
  50. 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.

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