NBI-921352, a first-in-class, NaV1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats.
Johnson JP, Focken T, Khakh K, Tari PK, Dube C, Goodchild SJ, Andrez JC, Bankar G, Bogucki D, Burford K, Chang E, Chowdhury S, Dean R, de Boer G, Decker S, Dehnhardt C, Feng M, Gong W, Grimwood M, Hasan A, Hussainkhel A, Jia Q, Lee S, Li J, Lin S, Lindgren A, Lofstrand V, Mezeyova J, Namdari R, Nelkenbrecher K, Shuart NG, Sojo L, Sun S, Taron M, Waldbrook M, Weeratunge D, Wesolowski S, Williams A, Wilson M, Xie Z, Yoo R, Young C, Zenova A, Zhang W, Cutts AJ, Sherrington RP, Pimstone SN, Winquist R, Cohen CJ, Empfield JR.
Johnson JP, et al.
Elife. 2022 Mar 2;11:e72468. doi: 10.7554/eLife.72468.
Elife. 2022.
PMID: 35234610
Free PMC article.
NBI-921352 is a potent inhibitor of Na(V)1.6 (IC(50)0.051 M), with exquisite selectivity over other sodium channel isoforms (selectivity ratios of 756 X for Na(V)1.1, 134 X for Na(V)1.2, 276 X for Na(V)1.7, and >583 Xfor Na(V)1.3, Na(V)1.4, and Na(V)1.5). ...
NBI-921352 is a potent inhibitor of Na(V)1.6 (IC(50)0.051 M), with exquisite selectivity over other sodium channel isoforms (selecti …