Sulfonamides as Selective Na(V)1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement

[Image: see text] Human genetic evidence has identified the voltage-gated sodium channel Na(V)1.7 as an attractive target for the treatment of pain. We initially identified naphthalene sulfonamide 3 as a potent and selective inhibitor of Na(V)1.7. Optimization to reduce biliary clearance by balancin...

Cijeli opis

Spremljeno u:
Bibliografski detalji
Izdano u:ACS Med Chem Lett
Glavni autori: Marx, Isaac E., Dineen, Thomas A., Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F., Du, Bingfan, Foti, Robert S., Fremeau, Robert T., Gao, Hua, Gunaydin, Hakan, Hall, Brian E., Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R., La, Daniel S., Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S., Moyer, Bryan D., Peterson, Emily A., Roberts, Jonathan T., Rose, Paul, Wang, Jean, Youngblood, Beth D., Yu, Violeta, Weiss, Matthew M.
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2016
Online pristup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5150675/
https://ncbi.nlm.nih.gov/pubmed/27994738
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00243
Oznake: Dodaj oznaku
Bez oznaka, Budi prvi tko označuje ovaj zapis!

Similar Items