The aim of this work was the preparation and characterization of nanodevices for the delivery of novel bifunctional σ1 ligands which have been showed to be a very promising tool for the treatment of neurodegenerative diseases. Compounds 1 and 2 were obtained by linking a natural antioxidant moiety, ALA, and an appropriate aminic moiety, based on the piperidine or piperazine scaffold. The interest for these compounds is due to their high affinity and selectivity for the σ1 receptors (Kiσ1 = 5.5 and 1.8 nM; Kiσ2/σ1 = 414 and 354, respectively), that have an important protective role against oxidative stress and neuronal apoptosis.
NANOENCAPSULATION FOR THE DELIVERY OF NOVEL BIFUNCTIONAL ANTIOXIDANT σ-1 SELECTIVE LIGANDS.
CARBONE, CLAUDIA;PREZZAVENTO, Orazio;
2015-01-01
Abstract
The aim of this work was the preparation and characterization of nanodevices for the delivery of novel bifunctional σ1 ligands which have been showed to be a very promising tool for the treatment of neurodegenerative diseases. Compounds 1 and 2 were obtained by linking a natural antioxidant moiety, ALA, and an appropriate aminic moiety, based on the piperidine or piperazine scaffold. The interest for these compounds is due to their high affinity and selectivity for the σ1 receptors (Kiσ1 = 5.5 and 1.8 nM; Kiσ2/σ1 = 414 and 354, respectively), that have an important protective role against oxidative stress and neuronal apoptosis.File in questo prodotto:
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