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.

Chelini, A., Brogi, S., Paolino, M., DI CAPUA, A., Cappelli, A., Giorgi, G., et al. (2017). Synthesis and Biological Evaluation of Novel Neuroprotective Pyridazine Derivatives as Excitatory Amino Acid Transporter 2 (EAAT2) Activators. JOURNAL OF MEDICINAL CHEMISTRY, 60(12), 5216-5221 [10.1021/acs.jmedchem.7b00383].

Synthesis and Biological Evaluation of Novel Neuroprotective Pyridazine Derivatives as Excitatory Amino Acid Transporter 2 (EAAT2) Activators

CHELINI, ALESSIA;PAOLINO, MARCO;DI CAPUA, ANGELA;CAPPELLI, ANDREA;GIORGI, GIANLUCA;ANZINI, MAURIZIO
2017

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.
Chelini, A., Brogi, S., Paolino, M., DI CAPUA, A., Cappelli, A., Giorgi, G., et al. (2017). Synthesis and Biological Evaluation of Novel Neuroprotective Pyridazine Derivatives as Excitatory Amino Acid Transporter 2 (EAAT2) Activators. JOURNAL OF MEDICINAL CHEMISTRY, 60(12), 5216-5221 [10.1021/acs.jmedchem.7b00383].
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11365/1012781