GABA Receptors

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  1. THIP

    Catalog No. A21738
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    δ-GABAAR agonist
    THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist. Learn More
  2. CTP354

    Catalog No. A15939
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    GABA(A) modulator
    CTP354 a novel deuterated subtype-selective GABA(A) modulator. Learn More
  3. Vigabatrin

    Catalog No. A15277
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    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. Learn More
  4. CP-409092

    Catalog No. A20152
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    GABAA receptor partial agonist
    CP-409092 is a partial agonist of GABAA receptor, with anti-anxiety activity. Learn More
  5. TPA 023

    Catalog No. A20140
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    GABAA α2/α3 agonist
    TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM. Learn More
  6. RWJ-51204

    Catalog No. A12875
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    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. Learn More
  7. MRK-016

    Catalog No. A12046
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    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. Learn More
  8. Gabazine

    Catalog No. A12627
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    GABAA receptor antagonist
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor. Learn More
  9. Acamprosate calcium

    Catalog No. A11308
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    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. Learn More
  10. (R)-Baclofen

    Catalog No. A16680
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    GABAB receptor agonist
    (R)-Baclofen(STX209) is a selective GABAB receptor agonist. Learn More
  11. L-655708

    Catalog No. A21181
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    GABAA receptor inverse agonist
    L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM). Learn More
  12. Basmisanil

    Catalog No. A21321
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    GABAAα5 modulator
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator. Learn More
  13. CP-409092 hydrochloride

    Catalog No. A21397
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    GABAA receptor partial agonist
    CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity. Learn More
  14. NS11394

    Catalog No. A21425
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    GABA(A) receptor modulator
    NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors. Learn More
  15. SCH 50911

    Catalog No. A21630
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    γ-Aminobutyric acid B GABA(B) receptor antagonist
    SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist. Learn More
  16. U-101017

    Catalog No. A13357
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    Benzodiazepine receptor/GABAA receptor agonist
    U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects. Learn More
  17. Gaboxadol hydrochloride

    Catalog No. A21730
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    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. Learn More
  18. Lorediplon

    Catalog No. A13449
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    GABAA receptor modulator
    Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, Learn More
  19. U-93631

    Catalog No. A16336
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    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. Learn More
  20. Tiagabine hydrochloride

    Catalog No. A16135
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    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. Learn More
  21. Bemegride

    Catalog No. A12298
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    Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning. Learn More
  22. Bamaluzole

    Catalog No. A17107
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    GABA receptor agonist
    Bamaluzole is a GABA receptor agonist. Learn More
  23. (-)-Securinine

    Catalog No. A17102
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    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. Learn More
  24. Cgp 52432

    Catalog No. A17140
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    GABA-A receptor antagonist
    Cgp 52432 is a GABA-A receptor antagonist. Learn More
  25. Afloqualone

    Catalog No. A17276
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    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. Learn More
  26. Homotaurine

    Catalog No. A17944
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    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. Learn More
  27. Baclofen

    Catalog No. A18248
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    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. Learn More
  28. CGP 36742

    Catalog No. A18666
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    GABAB receptor antagonist
    CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood?Cbrain barrier after peripheral administration, with an IC50 of 32?μM. CGP 36742 is useful in treatment of depression. Learn More
  29. Oxiracetam

    Catalog No. A14281
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    Oxiracetam is a cyclic derivative of gamma-aminobutyric acid (GABA). Learn More
  30. Baicalin

    Catalog No. A10121
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    HIV-1 production Inhibitor
    Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors. Learn More
  31. Nefiracetam (Translon)

    Catalog No. A10631
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    Nefiracetam is cognitive enhancer. It activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems. Learn More
  32. SKF 89976A HCl

    Catalog No. A10849
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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. Learn More
  33. Flumazenil

    Catalog No. A10397
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    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. Learn More
  34. Furosemide

    Catalog No. A10412
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    Furosemide is a non-competitive antagonist at GABAA receptors with ~ 100-fold greater selectivity for α6-containing receptors than α1-containing receptors. Learn More
  35. Gabapentin

    Catalog No. A10413
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    Gabapentin (Neurontin) is a pharmaceutical agent, specifically a GABA analogue. Learn More
  36. Gabapentin Hydrochloride

    Catalog No. A10414
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    Gabapentin Hydrochloride is a GABA analogue. Learn More
  37. Primidone (Mysoline)

    Catalog No. A10754
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    Primidone is an anticonvulsant. Potentiates GABAA receptor function. Learn More
  38. (+)-Bicuculline

    Catalog No. A12590
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    GABAA antagonist
    (+)-Bicuculline is a classical GABAA antagonist. Learn More
  39. AWD 131-138

    Catalog No. A13726
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    GABAA receptor agonist
    AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models. Learn More
  40. 2-Hydroxysaclofen

    Catalog No. A13696
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    GABAB receptors antagonist
    2-Hydroxysaclofen is a potent and selective antagonist at GABAB receptors. Learn More
  41. Bretazenil

    Catalog No. A13784
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    GABAA agonist
    Bretazenil, a benzodiazepine receptor partial agonist, as an adjunct in the prophylactic treatment of OP poisoning. Learn More
  42. Piperazine

    Catalog No. A16171
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    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. Learn More
  43. Cloflubicyne

    Catalog No. A13932
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    GABA antagonist
    Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide. Learn More
  44. a5IA

    Catalog No. A14343
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    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. Learn More
  45. RO 15-3890

    Catalog No. A14349
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    benzodiazepine receptor antagonist
    Ro 15-1788 is a benzodiazepine receptor antagonist. Learn More
  46. Indiplon

    Catalog No. A13769
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    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. Learn More
  47. Guvacine hydrochloride

    Catalog No. A13613
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    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). Learn More
  48. Muscimol

    Catalog No. A14005
    GABAA/GABAC agonist
    Muscimol is a full GABAA agonist and partial GABAC agonist. It binds GABAA on both high- and low-affinity sites (Kd = 10 and 270 nM, respectively), stimulating chloride efflux with an EC50 value of 200 nM. Learn More
  49. Muscimol hydrobromide

    Catalog No. A13459
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    GABA(A) receptor agonist
    Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure. Learn More
  50. 4-Aminobutyric acid

    Catalog No. A14934
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    4-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system. Learn More

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