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Bioisosteric Modification of To042: Synthesis and Evaluation of Promising Use‐Dependent Inhibitors of Voltage‐Gated Sodium Channels

Three analogues of To042, a tocainide‐related lead compound recently reported for the treatment of myotonia, were synthesized and evaluated in vitro as skeletal muscle sodium channel blockers possibly endowed with enhanced use‐dependent behavior. Patch‐clamp experiments on hNav1.4 expressed in HEK29...

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Detalles Bibliográficos
Autores principales: Milani, Gualtiero, Cavalluzzi, Maria Maddalena, Altamura, Concetta, Santoro, Antonella, Perrone, Mariagrazia, Muraglia, Marilena, Colabufo, Nicola Antonio, Corbo, Filomena, Casalino, Elisabetta, Franchini, Carlo, Pisano, Isabella, Desaphy, Jean‐François, Carrieri, Antonio, Carocci, Alessia, Lentini, Giovanni
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9293070/
https://www.ncbi.nlm.nih.gov/pubmed/34519427
http://dx.doi.org/10.1002/cmdc.202100496