Ontology highlight
ABSTRACT:
SUBMITTER: Sparling BA
PROVIDER: S-EPMC6072352 | biostudies-literature | 2017 Apr
REPOSITORIES: biostudies-literature
Sparling Brian A BA Yi S S Able J J Bregman H H DiMauro Erin F EF Foti R S RS Gao H H Guzman-Perez A A Huang H H Jarosh M M Kornecook T T Ligutti J J Milgram B C BC Moyer B D BD Youngblood B B Yu V L VL Weiss M M MM
MedChemComm 20161202 4
Na<sub>V</sub>1.7 is a particularly compelling target for the treatment of pain. Herein, we report the discovery and evaluation of a series of piperazine amides that exhibit state-dependent inhibition of Na<sub>V</sub>1.7. After demonstrating significant pharmacodynamic activity with early lead compound <b>14</b> in a Na<sub>V</sub>1.7-dependent behavioural mouse model, we systematically established SAR trends throughout each sector of the scaffold. The information gleaned from this modular anal ...[more]