Referenced in: none

Automatically associated channels: Nav1.5 , Nav1.7

Title: Discovery of pyrrolo-benzo-1,4-diazines as potent Na(v)1.7 sodium channel blockers.

Authors: Ginny D Ho, Deen Tulshian, Ana Bercovici, Zheng Tan, Jennifer Hanisak, Stephanie Brumfield, Julius Matasi, Charles R Heap, William G Earley, Brandy Courneya, R Jason Herr, Xiaoping Zhou, Terry Bridal, Diane Rindgen, Steve Sorota, Shu-Wei Yang

Journal, date & volume: Bioorg. Med. Chem. Lett., 2014 Sep 1 , 24, 4110-3

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25113934

Abstract
A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. Compound 41 displayed anti-nociceptive efficacy in the rat CFA pain model at 100 mpk oral dosing.