- 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.
- Seda Onder, .et al. , Chem Biol Interact, 2022, Aug 25;363:110029 PMID: 35779611
- Seham S El-Hawary, .et al. , Food Funct, 2022, Sep 7;12(17):8078-8089 PMID: 34286787
- Zsolt Datki, .et al. , Int J Biol Macromol, 2022, Jan 7;201:262-269 PMID: 34999044
- Suresh K.Bowroju, .et al. , Bioorg Med Chem, 2021, 45:116311
- Zsolt Datki, .et al. , Ecotoxicol Environ Saf, 2021, Jan 15;208:111666 PMID: 33396176
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Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
Gamma-secretase inhibitor
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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muscarinic receptor antagonist
5-hydroxymethyl tolterodine is a metabolite of Tolterodine, a muscarinic receptor antagonist used in the treatment of urinary incontinence.
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γ-secretase inhibitor
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. -
γ-secretase inhibitor
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . -
Gamma-secretase modulator
gamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for Alzheimer's disease. - Methoctramine hydrate is a selective M2 muscarinic receptor antagonist at nM concentrations
- Lingyu Wang, .et al. , Gut Microbes, 2020, 12(1): 1-20 PMID: 33006494
- 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.
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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. -
NMDA receptor antagonist
SDZ 220-581 is a competitive NMDA receptor antagonist (pKi = 7.7). -
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.- Chao Liu, .et al. , Cell Death Differ, 2018, Apr; 25(4): 661-676 PMID: 29238071
- Miglustat hydrochloride is an orally active α-glucosidase I and II and ceramide-specific glycosyltransferase inhibitor.
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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. - 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.
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COMT inhibitor
opicapone is a novel catechol-O-methyltransferase inhibitor -
NMDA receptors Blocker
Ro 25-6981 is a high-affinity, potent and selective blocker of N-methyl- D-aspartate (NMDA) receptors. -
CaM kinase II inhibitor
KN-93 is an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase.- Christian E Coleman, .et al. , Arch Microbiol, 2022, Jul 24;204(8):519 PMID: 35871646
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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. -
GABAA receptor modulator
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, -
GABA(A) receptor agonist
Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure. -
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. -
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). -
nAChR agonist
5-Iodo-A-85380 2HCl is a highly potent and subtype-selective agonist for the a4b2 and a6b2 nicotinic acetylcholine receptors. -
nAChR agonist
ABT-418 HCl is a neuronal nicotinic acetylcholine receptor agonist. -
GABAB receptors antagonist
2-Hydroxysaclofen is a potent and selective antagonist at GABAB receptors. -
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.- Tan YJ, .et al. , Future Med Chem, 2018, Sep 1;10(17):2039-2057 PMID: 30066578
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AChE inhibitor
Desoxypeganine hydrochloride is an AChE (acetylcholinesterase) inhibitor that has been used in the treatment of Alzheimer's dementia. -
GABA antagonist
Cloflubicyne is a potent non-competitive GABA antagonist, convulsant, laboratory insecticide. -
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. -
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.- Kazuki Yuasa, .et al. , Sci Rep, 2018, 8: 9037 PMID: 29899565
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BACE1 Inhibitor
Timosaponin B-II is a major active component of Anemarrhena asphodeloides Bunge (Liliaceae, rhizome) that has protective effects against cerebral ischaemic damage. - 4-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system.
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Glycine reuptake inhibitor
RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1). -
M1 agonist
Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.