Neuronal Signaling

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  1. muscarinic receptor antagonist

    SVT-40776 is a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder.
  2. γ-Secretase Inhibitor

    BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.
  3. neuronal nicotinic receptor agonist

    Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
  4. nAChR agonist

    (±)-Epibatidine is a nicotinic agonist. (±)-Epibatidine is a neuronal nAChR agonist.
  5. acetylcholine receptor antagonist

    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
  6. NMDAR modulator

    GNE 0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
  7. COX/5-LOX inhibitor

    Tepoxalin is a dual cyclooxygenase/5-lipoxygenase inhibitor of arachidonic acid metabolism with potent anti-inflammatory activity and a favorable gastrointestinal profile
  8. BF-168, a candidate probe for PET, is found to specifically recognize both neuritic and diffuse plaques, with a Ki of 6.4 nM for Aβ1-42.
  9. COX-1 inhibitor

    Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 ?M and 1.2 ?M for COX-1 and COX-2, respectively.
  10. 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.
  11. muscarinic M(3) receptor antagonist

    PF-3635659 is a potent muscarinic M(3) receptor antagonist.
  12. SPPL2a inhibitor

    SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
  13. nAChR agonist

    Sofinicline is a novel nicotinic acetylcholine receptor agonist in the treatment of attention-deficit/hyperactivity disorder.
  14. benzodiazepine receptor antagonist

    Ro 15-1788 is a benzodiazepine receptor antagonist.
  15. BACE1 inhibitor

    AMG-8718 is a potent and orally efficacious BACE1 inhibitor.
  16. gamma-secretase modulator

    gamma-secretase modulator 3 is a gamma-secretase modulator.
  17. Amyloid b-Peptide (1-43) (human), amyloid β peptide fragment. Highly toxic, showing higher neurotoxicity compared to Aβ40 and Aβ42.
  18. γ-Secretase inhibitor

    Z-Ile-Leu-aldehyde is a potent gamma-Secretase inhibitor; Notch signaling inhibitor.
  19. P2Y12 receptors inhibitor

    Cangrelor Tetrasodium is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. Unlike clopidogrel (Plavix), which is a prodrug, cangrelor is an active drug not requiring metabolic conversion.
  20. BACE1 inhibitor

    BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer's disease.
  21. M4 modulator

    VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
  22. α7 nAChR Modulator

    BNC375 is a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs.
  23. P2Y12 platelet inhibitor

    Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis.
  24. M1 modulator

    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
  25. AAK1 inhibitor

    LP-935509 is a potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1).
  26. γ-secretase modulator

    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively.
  27. BuChE inhibitor

    BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM.
  28. β-amyloid (Aβ) inhibitor

    ALZ-801 is an oral, small-molecule inhibitor of beta amyloid (Aβ) oligomer formation for Alzheimer's disease (AD). ALZ-801 is a prodrug of tramiprosate with improved pharmacokinetic properties and gastrointestinal tolerability.
  29. PQM130, a Feruloyl-Donepezil Hybrid compound with brain penatration, is a multitarget drug candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity. PQM130 acts as a neuroprotective compound for anti-AD drug development.
  30. BACE-1 inhibitor

    Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively.
  31. Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1.
  32. BACE1 inhibitor

    BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM.
  33. CaMK antagonist

    Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM.
  34. GlyT1 inhibitor

    GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC50 of 38 nM for rGlyT1. Antipsychotic activity.
  35. α1β3 GABA(A) receptor modulator

    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
  36. COX-1/COX-2 inhibitor

    (-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
  37. 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.
  38. Xanthocillin X permethyl ether is a natural compound isolated from fungal extracts, with Aβ-42 lowering activity.
  39. GlyT2 inhibitor

    ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model.
  40. BACE-1 inhibitor

    BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC50 of 56 nM.
  41. γ secretase modulator

    BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for Aβ42.
  42. glutaminyl cyclase inhibitor

    Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC50 of 1.23 μM.
  43. GluN2B modulator

    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  44. α4β2 nicotinic acetylcholine receptor partial agonist

    Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation.
  45. 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.
  46. P2X7R antagonist

    AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10?nM.
  47. GlyT1 inhibitor

    NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively.
  48. 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).
  49. BACE1 inhibitor

    PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
  50. GABAA receptor partial agonist

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

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