Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/6871
Title: Synthesis and Biological Evaluation of Novel Neuroprotective Pyridazine Derivatives as Excitatory Amino Acid Transporter 2 (EAAT2) Activators
Authors: CHELINI, ALESSIA
BROGI, SIMONE
Paolino, Marco 
DI CAPUA, ANGELA
Cappelli, Andrea 
Giorgi, Gianluca 
Farzad, Mersedeh
Di Cesare Mannelli, Lorenzo
Micheli, Laura
Ghelardini, Carla
Anzini, Maurizio 
Issue Date: 2017
Project: None 
Journal: JOURNAL OF MEDICINAL CHEMISTRY
Abstract: 
LDN-212320 (3) was found to be a potent EAAT2 activator at a translational level, restoring the normal clearance of glutamate and providing neuronal protection. Since the pharmacologic activation of EAAT2 represents a valuable strategy to relieve neuropathic pain, we synthesized novel activators (4a-f) of EAAT2. Among them 4f, analyzed in comparison with 3 by different paradigms in a rat model of oxaliplatin-induced neuropathic pain, showed the better antihypersensitive profile being able to fully counteract the oxaliplatin-induced neuropathy.
Description: 
204243
URI: http://hdl.handle.net/20.500.12779/6871
ISSN: 0022-2623
DOI: 10.1021/acs.jmedchem.7b00383
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