GABA Receptors

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  1. 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.
  2. GABAA receptor modulator

    Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator,
  3. 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).
  4. benzodiazepine1 (BZ1) receptor agonist

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

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

    AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
  7. 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.
  8. GABAA agonist

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

    Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide.
  11. Oxiracetam is a cyclic derivative of gamma-aminobutyric acid (GABA).
  12. 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.
  13. benzodiazepine receptor antagonist

    Ro 15-1788 is a benzodiazepine receptor antagonist.
  14. 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.
  15. GABA receptor agonist

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

    Cgp 52432 is a GABA-A receptor antagonist.
  17. 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.
  18. L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5??-phosphate-dependent aminitransferase in E.
  19. (-)-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.
  20. Chloride Channel/GABA Receptor blocker

    Picrotoxinin negatively modulate the action of GABA on GABAA receptors.
  21. 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.
  22. 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.
  23. BDZ receptor agonist

    S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for ?CGABA and +GABA respectively.
  24. GABAA receptor agonist

    Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  25. Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
  26. Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
  27. GABAA α5 inverse agonist

    RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively).
  28. GABAA α2/α3 agonist

    TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.
  29. GABAA receptor partial agonist

    CP-409092 is a partial agonist of GABAA receptor, with anti-anxiety activity.
  30. Rilmazafone is a water-soluble benzodiazepine prodrug that acts as a sedative and hypnotic neuropsychiatric agent.
  31. tranquilizer

    Uldazepam is a benzodiazepine derivative and can be used to treat patients with anxiety syndromes as tranquilizer.
  32. benzodiazepine receptor antagonist

    Sarmazenil is a benzodiazepine receptor antagonist.
  33. GABA transaminase inhibitor

    L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
  34. 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.
  35. 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.
  36. DSP-0565 is a strong, broad-spectrum anti-epileptic drug (AED) candidate with unique GABAergic function.
  37. Lotilaner is an insecticide (veterinary drug).
  38. Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm.
  39. 5-HT1 receptor modulator

    NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
  40. 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.
  41. GABAA α5 modulator

    ONO-8590580 is a GABAA α5 negative allosteric modulator.
  42. α1β3 GABA(A) receptor modulator

    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
  43. 4-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system.
  44. Anxiolytic anticonvulsant

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

    Etifoxine hydrochloride is potentiator of GABAA receptor function in cultured neurons.
  46. 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.
  47. anti-cancer agent

    Ginsenoside Rc, isolated from Panax ginseng, may exert various activities including anti-cancer, anti-inflammatory, antiobesity, and anti-diabetic effects.
  48. 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.
  49. 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.
  50. GABAB receptor agonist

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

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