220032-26-8Relevant articles and documents
Novel Multitarget-Directed Ligands (MTDLs) with Acetylcholinesterase (AChE) Inhibitory and Serotonergic Subtype 4 Receptor (5-HT4R) Agonist Activities As Potential Agents against Alzheimer's Disease: The Design of Donecopride
Rochais, Christophe,Lecoutey, Cédric,Gaven, Florence,Giannoni, Patrizia,Hamidouche, Katia,Hedou, Damien,Dubost, Emmanuelle,Genest, David,Yahiaoui, Samir,Freret, Thomas,Bouet, Valentine,Dauphin, Fran?ois,De Oliveira Santos, Jana S.,Ballandonne, Céline,Corvaisier, Sophie,Malzert-Fréon, Aurélie,Legay, Remi,Boulouard, Michel,Claeysen, Sylvie,Dallemagne, Patrick
, p. 3172 - 3187 (2015/04/27)
In this work, we describe the synthesis and in vitro evaluation of a novel series of multitarget-directed ligands (MTDL) displaying both nanomolar dual-binding site (DBS) acetylcholinesterase inhibitory effects and partial 5-HT4R agonist activity, among which donecopride was selected for further in vivo evaluations in mice. The latter displayed procognitive and antiamnesic effects and enhanced sAPPα release, accounting for a potential symptomatic and disease-modifying therapeutic benefit in the treatment of Alzheimer's disease. (Figure Presented).