Cognex (tacrine) / Shionogi 
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  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  N-alkylated Tacrine Derivatives as Potential Agents in Alzheimer's Disease Therapy. (Pubmed Central) -  Aug 4, 2020   
    Blood-brain barrier penetrating properties and effect on the viability of liver cells were determined as well. Rather than highlighting one particular derivative, this study points out more on the influence of an alkyl chain on different biological activities related to Alzheimer's disease.
  • ||||||||||  acetazolamide / Generic mfg., Cognex (tacrine) / Shionogi
    Journal:  Investigation of inhibitory properties of some hydrazone compounds on hCA I, hCA II and AChE enzymes. (Pubmed Central) -  Apr 14, 2020   
    N,N'-Bis[1-(4-fluorophenyl)-3-(piperidine-1-yl)propylidene]hydrazine dihydrochlorides, P7, was the most potent compound on AChE with the K value of 66 ± 20 nM. The other most promising compounds, N,N'-bis[1-(4-hydroxyphenyl)-3-(morpholine-4-yl)propylidene]hydrazine dihydrochlorides, N4 in N-series and N,N'-bis[1-(4-hydroxyphenyl)-3-(pyrrolidine-1-yl)propylidene]hydrazine dihydrochlorides, R4 in R-series were againts AChE with the K values of 119 ± 20 nM, 88 ± 14 nM, respectively.
  • ||||||||||  donepezil / Generic mfg., rivastigmine / Generic mfg.
    Journal:  Donepezil, a drug for Alzheimer's disease, promotes oligodendrocyte generation and remyelination. (Pubmed Central) -  Apr 14, 2020   
    More interestingly, donepezil also promotes the repair of the myelin sheaths in vivo and provides significant therapeutic effect in a cuprizone-mediated demyelination animal model. Donepezil is a drug that has been used to treat AD safely for many years; our findings suggest that it might be repurposed to treat CNS demyelinating diseases such as MS by promoting OPC to OL differentiation and remyelination.
  • ||||||||||  Imperan (metoclopramide) / Generic mfg.
    Review, Journal:  Reversible cholinesterase inhibitors as pretreatment for exposure to organophosphates. A review. (Pubmed Central) -  Apr 10, 2020   
    No correlation was observed between the IC of the reversible AChE inhibitors and their protective efficacy. These studies indicate that K-27 can be considered a very promising broad-spectrum prophylactic agent in case of imminent organophosphate exposure, which may be related to its AChE reactivating activity rather than its AChE inhibition.
  • ||||||||||  sarizotan (EMD128130) / Newron, Cognex (tacrine) / Shionogi
    Preclinical, Journal:  Non-dopaminergic Alterations in Depression-Like FSL Rats in Experimental Parkinsonism and L-DOPA Responses. (Pubmed Central) -  Apr 9, 2020   
    FSL rats showed a potentiated tremorgenic response to tacrine, a cholinesterase inhibitor used experimentally to induce 6 Hz resting tremor reminiscent of parkinsonian tremor...However, following chronic treatment with L-DOPA, FRL rats developed sensitization of turning and abnormal involuntary movements (AIMs); these effects were counteracted by the anti-dyskinetic 5-HT agonist/D partial agonist sarizotan...The marked behavioral difference between the FRL and FSL rats was paralleled with the striatal expression of the established marker, c-fos, but also the GABAergic transporter (vGAT), and a hitherto unknown marker, tamalin, that is known to regulate mGluR5 receptor function and postsynaptic organization. This study demonstrates that behavioral and transcriptional responses of non-dopaminergic systems to experimental parkinsonism and L-DOPA are modified in a genetic rat model of depression.
  • ||||||||||  donepezil / Generic mfg.
    Journal:  Mono- or di-substituted imidazole derivatives for inhibition of acetylcholine and butyrylcholine esterases. (Pubmed Central) -  Apr 1, 2020   
    ADME predictions revealed that the synthesized molecules might pass through the blood brain barrier and intestinal epithelial barrier and circulate freely in the blood stream without binding to human serum albumin. While the toxicity of one compound on the WS1 (skin fibroblast) cell line was 1790 µM, its toxicity on the SH-SY5Y (neuroblastoma) cell line was 950 µM.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Switching enzyme activity by a temperature responsive inhibitor modified polymer. (Pubmed Central) -  Mar 25, 2020   
    A thermoresponsive NIPAAm-based polymer is combined with the selective acetylcholinesterase inhibitor tacrine in order to create a strict in sense on/off switch for enzymatic activity. This polymer-inhibitor conjugate inhibits AChE at room temperature and enables reactivation of AChE by heating above the cloud point of the conjugate.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Biomarker, Journal:  A Potent Acetylcholinesterase Selective and Reversible Homodimeric Agent based on Tacrine for Theranostics. (Pubmed Central) -  Mar 18, 2020   
    Moreover, the bivalent ligand was also proven to be of neurogenic potential due to its ability to induce S-phase post-treatment in rat hippocampal neuronal cells. On the basis of initial results, the agent could be further explored for its theranostic value clinically, which gives the possibility of tracing the AChE levels by molecular imaging techniques in correlation with progression of neurocognitive disorders like Alzheimer's disease for better therapy response and patient management.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Preclinical, Journal:  Pig Skin Gelatin Hydrolysates Attenuate Acetylcholine Esterase Activity and Scopolamine-induced Impairment of Memory and Learning Ability of Mice. (Pubmed Central) -  Mar 13, 2020   
    Seventy male ICR mice weighing 20-25 g were randomly assigned to seven groups: Control (CON); scopolamine (SCO, 1 mg/kg B.W., intraperitoneally (i.p.); tetrahydroaminoacridine 10 [THA 10, tacrine; 10 mg/kg B.W. per oral (p.o.) with SCO (i.p.)]; PSW 10 (10 mg/kg B.W. (p.o.) with SCO (i.p.); PSW 40 (40 mg/kg B.W. (p.o.) with SCO (i.p.); LPSW 100 (100 mg/kg B.W. (p.o.) with SCO (i.p.); LPSW 400 (400 mg/kg B.W. (p.o.) with SCO (i.p.)...LPSW 100 and LPSW 400 reduced monoamine oxidase-B activity. These results indicated that LPSW at 400 mg/kg B.W. is a potentially strong antioxidant and contains novel components for the functional food industry.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Preclinical, Journal:  Colorimetric assay of acetylcholinesterase inhibitor tacrine based on MoO nanoparticles as peroxidase mimetics. (Pubmed Central) -  Mar 12, 2020   
    Based on these properties, a colorimetric assay method was developed for AChE inhibitor tacrine. This work not only broadens the application of the peroxidase mimetics, but also overcome the disadvantages of traditional methods such as expensive, complex and vulnerable to background interference for colorimetric assay of AChE inhibitor.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Two New AChE Inhibitors Isolated from Li Folk Herb Heilaohu "Kadsura coccinea" Stems. (Pubmed Central) -  Feb 15, 2020   
    Their structures were elucidated by comprehensive analyses of mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopic data. To search healthy components, an acetylcholinesterase (AChE) inhibitory activity test by Ellman's Method was conducted, kadsuricoccins A and B showed activity with the AChE inhibit index (AII) up to 68.96% ± 0.19% and 57.8% ± 0.11% at 94 nM (compared with positive control tacrine AII 79.80% ± 0.20%, 9.4 nM), respectively.
  • ||||||||||  ciprofloxacin / Generic mfg.
    Journal:  Alteration of mitochondrial DNA homeostasis in drug-induced liver injury. (Pubmed Central) -  Feb 14, 2020   
    Lastly, some drugs might alter the mtDNA methylation status but the pathophysiological consequences of such alteration are still unclear. Drug-induced impairment of mtDNA homeostasis is probably under-recognized since preclinical and post-marketing safety studies do not classically investigate mtDNA levels, mitochondrial protein synthesis and mtDNA oxidative damage.
  • ||||||||||  donepezil / Generic mfg.
    Clinical, Journal:  The high efficacy of muscarinic M4 receptor in D1 medium spiny neurons reverses striatal hyperdopaminergia. (Pubmed Central) -  Jan 25, 2020   
    In vivo experiments with acetylcholinesterase inhibitors donepezil and tacrine, as well as with the positive allosteric modulators of M receptor VU0152100 and VU0010010 show that this effect is sufficient to reverse the increased locomotor activity of DAT-knockout mice. This suggests that M receptors could be a novel therapeutic target to treat hyperactivity disorders.
  • ||||||||||  donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
    Journal:  Synthesis of 2-(2-oxo-2H-chromen-4-yl)acetamides as potent acetylcholinesterase inhibitors and molecular insights into binding interactions. (Pubmed Central) -  Jan 23, 2020   
    The most active compound in this series, 5a (IC 0.04 ± 0.01 µM), noncompetitively inhibited AChE with a higher potency than tacrine and galantamine...Molecular docking was applied to postulate the selectivity toward AChE of 5a in comparison with donepezil and tacrine...ADMET analysis suggested that the 2-(2-oxo-2H-chromen-4-yl)acetamides showed a good pharmacokinetic profile and no hepatotoxicity. These coumarin derivatives showed high potential for further development as anti-Alzheimer agents.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Annona atemoya Leaf Extract Improves Scopolamine-Induced Memory Impairment by Preventing Hippocampal Cholinergic Dysfunction and Neuronal Cell Death. (Pubmed Central) -  Dec 29, 2019   
    Fifty-eight mice were randomly divided into six groups and orally treated with AAL extract at (50, 100, or 200 mg/kg) or tacrine (TAC) for 21 days...Our findings demonstrate that AAL extract has the ability to alleviate memory impairment through preventative effect on cholinergic system dysfunction and oxidative stress-related neuronal cell death in a SCO-induced memory deficit animal model. Overall, AAL may be a promising plant resource for the managing memory dysfunction due to neurodegenerative diseases, such as Alzheimer's disease (AD).
  • ||||||||||  Cognex (tacrine) / Shionogi
    Journal:  Simultaneous induction and blockade of autophagy by a single agent. (Pubmed Central) -  Dec 21, 2019   
    We demonstrate that tacrine-melatonin heterodimer C10, a potent anti-Alzheimer's disease drug, has an antiproliferative effect on MCF-7 breast cancer cells...We demonstrate that the same effect may be achieved using a single agent, C10. Our findings offer a new, promising strategy for anticancer treatment.
  • ||||||||||  donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
    Journal:  Cholinesterase as a Target for Drug Development in Alzheimer's Disease. (Pubmed Central) -  Nov 28, 2019   
    Herein, we describe the role of acetylcholine sterase (AChE) and related hypothesis in AD along with the pharmacological and chemical aspects of the available cholinesterase inhibitors. This chapter discusses the development of several congeners and hybrids of available cholinesterase inhibitors along with their binding patterns in enzyme active sites.
  • ||||||||||  Cognex (tacrine) / Shionogi
    Review, Journal:  Multifunctional properties of novel tacrine congeners: cholinesterase inhibition and cytotoxic activity. (Pubmed Central) -  Oct 31, 2019   
    This review describes the synthesis of a wide range of novel tetrahydroacridine derivatives (tiocyanates, selenocyanates, ureas, selenoureas, thioureas, isothioureas, disulfides, diselenides and several tacrine homo- and hetro-hybrids). These tacrine congeners exhibit significant anticholinesterase and cytotoxic properties and may therefore be of considerable potential for the development of new drugs for the treatment of Alzheimer's disease.