Referenced in: none

Automatically associated channels: Kv11.1 , Nav1.7

Title: N-Aryl azacycles as novel sodium channel blockers.

Authors: Stephen M Lynch, Laykea Tafesse, Kevin Carlin, Parijat Ghatak, Bin Shao, Haissam Abdelhamid, Donald J Kyle

Journal, date & volume: Bioorg. Med. Chem. Lett., 2015 Jan 1 , 25, 48-52

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25435147

Abstract
We have identified a new series of N-aryl azacycles as sodium channel blockers, which showed good potency on Nav1.7 in FLIPR-based and electrophysiological functional assays. Analogs from this series possessed selectivity over hERG, reasonable oral exposure in rat PK studies and are predicted to have limited CNS penetration.