GABA Receptors

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  1. 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.
  2. 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.
  3. 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).
  4. 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.
  5. 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.
  6. DSP-0565 is a strong, broad-spectrum anti-epileptic drug (AED) candidate with unique GABAergic function.
  7. Lotilaner is an insecticide (veterinary drug).
  8. Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm.
  9. 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.
  10. GABAA α5 modulator

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

    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
  12. 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.
  13. GABAA receptor agonist

    Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  14. 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.
  15. 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.
  16. 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).
  17. GABAA α2/α3 agonist

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

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

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

    Sarmazenil is a benzodiazepine receptor antagonist.
  22. 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.
  23. 4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyric acid (GABA) derivative.
  24. GABA receptor agonist

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

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

    Ru-32514 is an agonist of benzodiazepine receptor.
  27. 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.
  28. chemoprotective agent

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

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

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

    CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity.
  32. 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.
  33. 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.
  34. partial benzodiazepine receptor agonist

    Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity.
  35. 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.
  36. δ-GABAAR agonist

    THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist.
  37. Benzodiazepine inverse agonist

    DMCM (hydrochloride) is Benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity.
  38. GABAB receptor positive allosteric modulator

    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
  39. GABA-A modulator

    Imidazenil is a GABA-A modulator that blocks the sedative effects without lowering the convulsion threshold.
  40. nervoussystem toxicant

    Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects.
  41. benzodiazepine receptor agonist

    Cgs 20625 is a benzodiazepine receptor agonist.
  42. benzodiazepine receptor inverse agonist

    Ro 19-4603 is a benzodiazepine receptor inverse agonist.
  43. positive allosteric modulator of different isoforms of the GABAA receptor

    SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.
  44. GABA receptor antagonist

    Gabazine free base is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites.
  45. pyrazolopyridine anxiolytic

    Tracazolate is a pyrazolopyridine anxiolytic known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases.
  46. modulator of the GABAA receptor complex

    GABAA Modulator I is novel modulator of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
  47. GABAB receptor agonist

    rac-BHFF is a selective GABAB receptor agonist.

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