2026-06-27T10:30:45Zhttps://docta.ucm.es/rest/oai/request

oai:docta.ucm.es:20.500.14352/1204012025-05-22T23:46:37Zcom_20.500.14352_14col_20.500.14352_15

Romero Martínez, Manuel Alejandro Marco Contelles, José Luis Ramos Alonso, Eva 2025-05-22T14:19:23Z 2025-05-22T14:19:23Z 2020-01 Romero, A., Marco-Contelles, J., & Ramos, E. (2020). Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy. Neural regeneration research, 15(1), 30–35. https://doi.org/10.4103/1673-5374.262679 1673-5374 10.4103/1673-5374.262679 https://hdl.handle.net/20.500.14352/120401 1876-7958 https://doi.org/10.4103/1673-5374.262679 31535639 There is no effective treatment to face Alzheimer's disease complexity. Multitarget molecules are a good approach against the multiple physiopathological events associated with its development and progression. In this context, N-((5-(3-(1-benzylpiperidin-4-yl) propoxy)-1- methyl-1H-indol-2-yl)methyl)-N-methylprop-2-yn-1-amine (ASS234) has been tested achieving promising results. ASS234 has demonstrated to cross the blood-brain barrier in vivo, and a good in silico safety profile being less toxic than donepezil. Besides, ASS234 reversibly inhibits human acetyl- and butyryl-cholinesterase, and irreversibly inhibits human monoamine oxidase A and B. Moreover, this multitarget molecule has antioxidant and neuroprotective properties, and inhibits Αβ and Αβ self-aggregation. Inquiring about the mechanism of action, several signaling pathways related to Alzheimer's disease had been explored showing that ASS234 induces the wingless-type MMTV integration site (Wnt) family and several members of the heat shock proteins family and moreover counteracts neuroinflammatory and oxidative stress-related genes promoting the induction of several key antioxidant genes. Finally, in vivo experiments with ASS234 in C57BL/6J mice displayed its ability to reduce amyloid plaque burden and gliosis in the cortex and hippocampus, ameliorating scopolamine-induced learning deficits. Here we gather the information regarding ASS234 evaluated so far, showing its ability to face different targets, necessary to counteract a neurodegenerative disease as complex as the Alzheimer's disease. eng http://creativecommons.org/licenses/by-nc-nd/4.0/ open access Attribution-NonCommercial-NoDerivatives 4.0 International Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy. journal article