GABA Receptors

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  1. 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).
  2. GABAA antagonist

    (+)-Bicuculline is a classical GABAA antagonist.
  3. GABA(A) receptor agonist

    Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure.
  4. HIV-1 production Inhibitor

    Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.
  5. Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
  6. Benzodiazepine receptor agonist

    Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
  7. 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.
  8. 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.
  9. GABA reuptake inhibitor

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

    U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.
  11. 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.
  12. 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.
  13. 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.
  14. GABAA receptor modulator

    Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator,
  15. 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).
  16. benzodiazepine1 (BZ1) receptor agonist

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

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

    AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
  19. 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.
  20. GABAA agonist

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

    Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide.
  23. Oxiracetam is a cyclic derivative of gamma-aminobutyric acid (GABA).
  24. 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.
  25. benzodiazepine receptor antagonist

    Ro 15-1788 is a benzodiazepine receptor antagonist.
  26. GABA(A) modulator

    CTP354 a novel deuterated subtype-selective GABA(A) modulator.
  27. 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.
  28. 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.
  29. 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.
  30. GABAB receptor agonist

    (R)-Baclofen(STX209) is a selective GABAB receptor agonist.
  31. 4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyric acid (GABA) derivative.
  32. GABA receptor agonist

    Isoguvacine hydrochloride is a GABA receptor agonist.
  33. GABAA(α2/3) receptor modulator

    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
  34. GABA Receptor agonist

    Ru-32514 is an agonist of benzodiazepine receptor.
  35. 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.
  36. chemoprotective agent

    Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
  37. GABAA receptor inverse agonist

    L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM).
  38. GABAAα5 modulator

    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  39. GABAA receptor partial agonist

    CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity.
  40. 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.
  41. 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.
  42. GABAA receptor agonist

    Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  43. 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.
  44. 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.
  45. 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).
  46. GABAA α2/α3 agonist

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

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

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

    Sarmazenil is a benzodiazepine receptor antagonist.

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