scholarly journals Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment

Molecules ◽  
2010 ◽  
Vol 15 (12) ◽  
pp. 8804-8812 ◽  
Author(s):  
Jan Korabecny ◽  
Kamil Musilek ◽  
Ondrej Holas ◽  
Eugenie Nepovimova ◽  
Daniel Jun ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitor ◽  
Disease Treatment ◽  
In Vitro Evaluation

scholarly journals Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1626
Author(s):  
Line Séguy ◽  
Léna Guyon ◽  
Manon Maurel ◽  
Pascal Verdié ◽  
Audrey Davis ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
In Vitro Assays ◽  
Titration Calorimetry ◽  
Therapeutic Effects ◽  
Disease Treatment ◽  
Cellular Effects ◽  
Irritable Bowel ◽  
The Stability

Background and Purpose: The activation of 5-HT4 receptors with agonists has emerged as a valuable therapeutic strategy to treat Alzheimer’s disease (AD) by enhancing the nonamyloidogenic pathway. Here, the potential therapeutic effects of tegaserod, an effective agent for irritable bowel syndrome, were assessed for AD treatment. To envisage its efficient repurposing, tegaserod-loaded nanoemulsions were developed and functionalized by a blood–brain barrier shuttle peptide. Results: The butyrylcholinesterase inhibitory activity of tegaserod and its neuroprotective cellular effects were highlighted, confirming the interest of this pleiotropic drug for AD treatment. In regard to its drugability profile, and in order to limit its peripheral distribution after IV administration, its encapsulation into monodisperse lipid nanoemulsions (Tg-NEs) of about 50 nm, and with neutral zeta potential characteristics, was performed. The stability of the formulation in stock conditions at 4 °C and in blood biomimetic medium was established. The adsorption on Tg-NEs of peptide-22 was realized. The functionalized NEs were characterized by chromatographic methods (SEC and C18/HPLC) and isothermal titration calorimetry, attesting the efficiency of the adsorption. From in vitro assays, these nanocarriers appeared suitable for enabling tegaserod controlled release without hemolytic properties. Conclusion: The developed peptide-22 functionalized Tg-NEs appear as a valuable tool to allow exploration of the repurposed tegaserod in AD treatment in further preclinical studies.

[P1-039]: IN VITRO EVALUATION OF BENZOTHIAZOLE-BASED UREAS AS POTENTIAL ABAD/17β-HSD10 MODULATORS FOR ALZHEIMER'S DISEASE THERAPEUTICS

2017 ◽  
Vol 13 (7S_Part_5) ◽  
pp. P249-P249 ◽  
Author(s):  
Laura Aitken ◽  
Lukas Hroch ◽  
Rebecca Hughes ◽  
Thijs S. Udo ◽  
Ondrej Benek ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
In Vitro Evaluation

Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer’s disease

2020 ◽  
Vol 198 ◽  
pp. 112368 ◽  
Author(s):  
Julio Rodríguez-Lavado ◽  
Carlos Gallardo-Garrido ◽  
Michael Mallea ◽  
Victor Bustos ◽  
Rodrigo Osorio ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Molecular Docking ◽  
In Vitro Evaluation ◽  
New Class

scholarly journals A Snapshot on the Current Status of Alzheimer’s Disease, Treatment Perspectives, in-Vitro and in-Vivo Research Studies and Future Opportunities

2019 ◽  
Vol 67 (10) ◽  
pp. 1030-1041
Author(s):  
Gizem Tezel ◽  
Selin Seda Timur ◽  
İsmail Bozkurt ◽  
Ö. Faruk Türkoğlu ◽  
İpek Eroğlu ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Current Status ◽  
Disease Treatment ◽  
Research Studies

scholarly journals Design, Synthesis and in vitro Evaluation of Indolotacrine Analogues as Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease

ChemMedChem ◽  
2015 ◽  
Vol 11 (12) ◽  
pp. 1264-1269 ◽  
Author(s):  
Ondrej Benek ◽  
Ondrej Soukup ◽  
Marketa Pasdiorova ◽  
Lukas Hroch ◽  
Vendula Sepsova ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Design Synthesis ◽  
In Vitro Evaluation
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