Douglas Pereira Pinto, Diego de Sá Coutinho, Katharinne Ingrid Moraes de Carvalho, Maximiliano R Ferrero, Letícia Vallim da Silva, Gabriel Parreiras Estolano Silveira, Diego Medeiros da Silva, João Felipe Garcia Araújo, Aline C A Silva, Heliana Martins Pereira, Laís Bastos da Fonseca, Robson Xavier Faria, Marcus Vinicius Nora de Souza, Emerson Teixeira da Silva, Osvaldo Andrade Santos-Filho, Jorge Carlos Santos da Costa, Fábio Coelho Amendoeira, Marco Aurélio Martins
Existing evidence suggests that the local anaesthetic mexiletine can be beneficial for patients with asthma. However, caution is required since anaesthesia of the airways inhibits protective bronchodilator neuronal reflexes, limiting applications in conditions of hyperirritable airways. Here, we describe the synthesis of a new series of mexiletine analogues, which were screened for reduced activity in Na+ channels and improved smooth muscle relaxant effects, that were evaluated using the patch-clamp technique and an isolated tracheal organ bath, respectively...
August 1, 2020: European Journal of Pharmacology