Neuronal Signaling

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  1. Amyloid beta (Aβ or Abeta) is a peptide of 36-C43 amino acids that is processed from the Amyloid precursor protein. Amyloid β-Peptide (1-42) human is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
  2. Gamma-secretase inhibitor

    BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis.
  3. Gamma-secretase inhibitor

    RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.
  4. nAChR partial agonist

    Varenicline is a nicotinic receptor partial agonist.
  5. muscarinic receptor antagonist

    5-hydroxymethyl tolterodine is a metabolite of Tolterodine, a muscarinic receptor antagonist used in the treatment of urinary incontinence.

  6. Gamma-secretase inhibitor

    MK-0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated.
  7. γ-secretase inhibitor

    Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
  8. γ-secretase inhibitor

    PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM .
  9. Gamma-secretase modulator

    gamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for Alzheimer's disease.
  10. P2X1 antagonist

    NF279 is a suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC50/KB ~ 1 μM in smooth muscle).
  11. Methoctramine hydrate is a selective M2 muscarinic receptor antagonist at nM concentrations
  12. ATB-337 is a hybrid molecule of an H2S donor and the NSAID diclofenac
  13. Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.
  14. mAChR agonist

    AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
  15. BACE1 inhibitor

    Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
  16. NMDA receptor antagonist

    SDZ 220-581 is a competitive NMDA receptor antagonist (pKi = 7.7).
  17. γ-secretase inhibitor

    BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.
  18. Miglustat hydrochloride is an orally active α-glucosidase I and II and ceramide-specific glycosyltransferase inhibitor.
  19. BACE1 inhibitor

    AZD3839 is a potent and selective inhibitor of human BACE1 with Ki of 26.1 nM.
  20. 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.
  21. alpha-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam derived PKC activator (Ki = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblas.
  22. COMT inhibitor

    opicapone is a novel catechol-O-methyltransferase inhibitor
  23. NMDA receptors Blocker

    Ro 25-6981 is a high-affinity, potent and selective blocker of N-methyl- D-aspartate (NMDA) receptors.
  24. Gamma-secretase modulator

    TC-E 5006 is a gamma-secretase modulator. Reduces Aβ42 levels in vitro (EC50 = 390 nM) and in vivo.
  25. nonsteroidal glucocorticoid receptor agonist

    AZD5423 is a novel nonsteroidal glucocorticoid receptor agonist.
  26. CaM kinase II inhibitor

    KN-93 is an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase.
  27. NMDA receptor antagonist.

    (-)-MK 801 maleate acts as a potent, selective, and non-competitive NMDA receptor antagonist. It acts by binding to a site located within the NMDA associated ion channel.
  28. eEF2K (CAMKIII) inhibitor

    A-484954 is a potent, selective inhibitor of eukaryotic longation factor-2 kinase (eEF2K).
  29. GABAA receptor modulator

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

    Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure.
  31. α7 nAChR agonist

    A-582941 is a selective AChR a7 partial agonist. It exhibits high affinity for both rat and human a7 receptors (Ki values are 10.8 and 16.7 nM, respectively).
  32. NMDAR modulator

    GLYX-13 is a selective weak partial agonist of the glycine site of the NMDA receptor which is under development by Naurex as adjunctive therapy for treatment-resistant depression.
  33. 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).
  34. nAChR agonist

    5-Iodo-A-85380 2HCl is a highly potent and subtype-selective agonist for the a4b2 and a6b2 nicotinic acetylcholine receptors.
  35. nAChR agonist

    ABT-418 HCl is a neuronal nicotinic acetylcholine receptor agonist.
  36. GABAB receptors antagonist

    2-Hydroxysaclofen is a potent and selective antagonist at GABAB receptors.
  37. NMDA receptor antagonist

    MDL-29951 is a novel glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) in vitro and in vivo.
  38. Gamma-secretase inhibitor

    FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.
  39. AChE inhibitor

    Desoxypeganine hydrochloride is an AChE (acetylcholinesterase) inhibitor that has been used in the treatment of Alzheimer's dementia.
  40. GABA antagonist

    Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide.
  41. NMDA& mGlu receptor agonist

    Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist.
  42. M2/M4 AChR agonist

    LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
  43. CaMKII inhibitor

    KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities.
  44. 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.
  45. BACE1 Inhibitor

    Timosaponin B-II is a major active component of Anemarrhena asphodeloides Bunge (Liliaceae, rhizome) that has protective effects against cerebral ischaemic damage.
  46. Peimisine and peiminine production by endophytic fungus Fusarium sp. isolated from Fritillaria unibracteata var. wabensis.
  47. 4-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system.
  48. Glycine reuptake inhibitor

    RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).
  49. M1 agonist

    Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
  50. CaMK-II Inhibitor

    KN-92 hydrochloride is a negative control for KN-93.

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